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Purity: ≥98%
Dalbavancin HCl (MDL-63397; BI-397; A-A 1; VER-001; Dalvance; Xydalba), a semisynthetic lipoglycopeptide, is a novel, potent and second-generation lipoglycopeptide antibiotic active against gram-positive pathogens. It is in the same class as vancomycin which is the most widely used and one of the few treatments available to patients infected with methicillin-resistant Staphylococcus aureus (MRSA). Dalbavancin was designed based on vancomycin and teicoplanin. It possesses in vitro activity against a variety of Gram-positive pathogens including MRSA and methicillin-resistant Staphylococcus epidermidis (MRSE).
| Targets |
Glycopeptide
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|---|---|
| ln Vitro |
Dalbavancin is a semisynthetic lipoglycopeptide that is administered intravenously and was created to treat infections brought on by pathogens that are resistant to antibiotics. Strong in vitro bactericidal activity is demonstrated by dalapancin against gram-positive pathogens such as non-VanA strains of VRE, VISA, and S. aureus (MRSA). Dalbavancin has demonstrated greater potency against MRSA and β-hemolytic streptococci than other glycopeptide therapeutic agents, making it an excellent treatment for complicated skin and skin structure infections (cSSSIs)[1][2].
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| ln Vivo |
Treatment with dalapancin (15–240 mg/kg; intraperitoneal injection; every 36 or 72 hours; for 14 days; female BALB/c mice) results in an 80%–100% survival rate across all dose regimens[1].
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| Animal Protocol |
Animal Model: Female BALB/c mice (6-8 weeks) challenged with Ames strain of B. anthracis[1]
Dosage: 15 mg/kg, 30 mg/kg, 60 mg/kg, 120 mg/kg, 240 mg/kg Administration: Intraperitoneal injection; every 36 h or 72 h; for 14 days Result: Treatment started 24 hours after the challenge, with regimens of 15 to 120 mg/kg every 36 hours or 30 to 240 mg/kg every 72 hours. The rate of survival at 42 days showed an 80 to 100% efficacy. |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
In healthy subjects, dalbavancin AUC0-24h and Cmax both increased proportionally to dose following single intravenous (IV) dalbavancin doses ranging from 140 mg to 1500 mg, indicating linear pharmacokinetics. No apparent accumulation of dalbavancin was observed following multiple IV infusions administered once weekly for up to eight weeks, with 1000 mg on Day 1 followed by up to seven weekly 500 mg doses, in healthy adults with normal renal function. Following administration of a single 1000 mg dose in healthy subjects, an average of 33% of the administered dalbavancin dose was excreted in urine as unchanged dalbavancin and approximately 12% of the administered dose was excreted in urine as the metabolite hydroxy-dalbavancin through 42 days post-dose. Approximately 20% of the administered dose was excreted in feces through 70 days post-dose. Clearance and volume of distribution at steady state are comparable between healthy subjects and patients with infections. The volume of distribution at steady state was similar to the volume of extracellular fluid. 0.0513 L/h. Metabolism / Metabolites Dalbavancin is not a substrate, inhibitor, or inducer of CYP450 isoenzymes. Subsequently, metabolites have not been observed in significant amounts in human plasma. The metabolites hydroxy-dalbavancin and mannosyl aglycone have been detected in urine (< 25% of administered dose). The metabolic pathways responsible for producing these metabolites have not been identified; however, due to the relatively minor contribution of metabolism to the overall elimination of dalbavancin, drug-drug interactions via inhibition or induction of metabolism of dalbavancin are not anticipated. Hydroxy-dalbavancin and mannosyl aglycone show significantly less antibacterial activity compared to dalbavancin. Biological Half-Life Terminal half life is 346 hours. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Dalbavancin is 93% plasma protein bound and is poorly absorbed orally, so it is not likely to reach the bloodstream of the infant or cause any adverse effects in breastfed infants. If dalbavancin is required by the mother, it is not a reason to discontinue breastfeeding. Monitor the infant for possible effects on the gastrointestinal tract, such as diarrhea, vomiting, and candidiasis (e.g., thrush, diaper rash). ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. Protein Binding Dalbavancin is reversibly bound to human plasma proteins, primarily to albumin. The plasma protein binding of dalbavancin is 93% and is not altered as a function of drug concentration, renal insufficiency, or hepatic insufficiency. |
| References |
[1]Antimicrob Agents Chemother. 2010 Mar;54(3):991-6.; [2]Ther Clin Risk Manag. 2008 Feb;4(1):31-40. [3]Clin Drug\nInvestig. 2015 Oct 12. PubMed PMID: 26458939. [4]J Antimicrob\nChemother. 2015 Oct 7. pii: dkv303. PMID:\n26451012. [5]Antimicrob Agents Chemother. 2015 Sep 21.\npii: AAC.01717-15. [6]J Vis Exp. 2015 Sep 9;(103).\ndoi: 10.3791/53028. PubMed PMID: 26381422. |
| Additional Infomation |
Pharmacodynamics
The antibacterial activity of dalbavancin appears to best correlate with the ratio of area under the concentration-time curve to minimal inhibitory concentration (AUC/MIC) for Staphylococcus aureus based on animal models of infection. An exposure-response analysis of a single study in patients with complicated skin and skin structure infections supports the two-dose regimen for which dalbavancin injection is administered. Subsequently, the recommended dosage regimen of dalbavancin in patients with normal renal function is 1500 mg, administered either as a single dose, or 1000 mg followed one week later by 500 mg [FDA Label, F2356. Dalbavancin should be administered over 30 minutes by intravenous infusion. Furthermore, inn a randomized, positive- and placebo-controlled, thorough QT/QTc study, 200 healthy subjects received either dalbavancin 1000 mg intravenous (IV), dalbavancin 1500 mg IV, oral moxifloxacin 400 mg, or placebo. Neither dalbavancin 1000 mg nor dalbavancin 1500 mg had any clinically relevant adverse effect on cardiac repolarization. |
| Molecular Formula |
C88H100N10O28CL2
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|---|---|
| Molecular Weight |
1816.6918
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| Exact Mass |
1814.608
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| CAS # |
171500-79-1
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| Related CAS # |
Dalbavancin hydrochloride;2227366-51-8;Dalbavancin-d6;1126461-54-8
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| PubChem CID |
16134627
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.6±0.1 g/cm3
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| Index of Refraction |
1.729
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| LogP |
2.94
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| Hydrogen Bond Donor Count |
21
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| Hydrogen Bond Acceptor Count |
30
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| Rotatable Bond Count |
22
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| Heavy Atom Count |
128
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| Complexity |
3740
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| Defined Atom Stereocenter Count |
18
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| SMILES |
O[C@@H]([C@@H](O)[C@@H]1O)[C@H](O[C@@H]1CO)OC2=C(C3=CC([C@@](C4=O)([H])NC([C@@](NC([C@](NC([C@@](NC5=O)([H])C6)=O)([H])C(C=C7OC(C=C8[C@H]5NC)=C(C=C8)O)=C(C(O)=C7)Cl)=O)([H])C9=CC%10=C(O[C@H](O[C@H](C(O)=O)[C@@H](O)[C@@H]%11O)[C@@H]%11NC(CCCCCCCCC(C)C)=O)C(OC%12=CC=C6C=C%12)=C9)=O)=CC=C3O)C([C@@](NC([C@](N4)([H])[C@@H](C%13=CC=C(O%10)C(Cl)=C%13)O)=O)([H])C(NCCCN(C)C)=O)=CC(O)=C2
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| InChi Key |
KGPGQDLTDHGEGT-SZUNQUCBSA-N
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| InChi Code |
InChI=1S/C88H100Cl2N10O28/c1-38(2)13-10-8-6-7-9-11-14-61(106)94-70-73(109)75(111)78(86(120)121)128-87(70)127-77-58-31-43-32-59(77)124-55-24-19-42(29-50(55)89)71(107)69-85(119)98-67(80(114)92-25-12-26-100(4)5)48-33-44(102)34-57(125-88-76(112)74(110)72(108)60(37-101)126-88)62(48)47-28-40(17-22-52(47)103)65(82(116)99-69)95-83(117)66(43)96-84(118)68-49-35-46(36-54(105)63(49)90)123-56-30-41(18-23-53(56)104)64(91-3)81(115)93-51(79(113)97-68)27-39-15-20-45(122-58)21-16-39/h15-24,28-36,38,51,60,64-76,78,87-88,91,101-105,107-112H,6-14,25-27,37H2,1-5H3,(H,92,114)(H,93,115)(H,94,106)(H,95,117)(H,96,118)(H,97,113)(H,98,119)(H,99,116)(H,120,121)/t51-,60-,64-,65-,66-,67+,68+,69+,70-,71-,72-,73-,74+,75+,76+,78+,87-,88+/m1/s1
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| Chemical Name |
Ristomycin A aglycone, 5,31-dichloro-38-de(methoxycarbonyl)-7-demethyl-19-deoxy-56-O-(2-deoxy-2-((10-methyl-1-oxoundecyl)amino)-beta-D-glucopyranuronosyl)-38-(((3-(dimethylamino)propyl)amino)carbonyl)-42-O-alpha-D-mannopyranosyl-N15-methyl-
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| Synonyms |
MDL-63397; MDL 63397; BI-397; VER001; MDL63397;A-A 1; BI397; BI 397; VER 001; VER-001; MDL 63397; Dalbavancin. Dalbavancin B0;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL ( ~55.04 mM )
Water : ~100 mg/mL
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5505 mL | 2.7523 mL | 5.5045 mL | |
| 5 mM | 0.1101 mL | 0.5505 mL | 1.1009 mL | |
| 10 mM | 0.0550 mL | 0.2752 mL | 0.5505 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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