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Purity: ≥98%
AMY-101 (also known as Cp40) is a peptidic inhibitor of the central complement component C3. Locally administered AMY-101 (Cp40) can inhibit naturally occurring periodontitis in non-human primates (NHPs) when given once a week. Moreover, a daily subcutaneous dose of AMY-101 (4 mg/kg bodyweight) was protective against NHP periodontitis, suggesting that patients treated for systemic disorders (e.g., paroxysmal nocturnal hemoglobinuria) can additionally benefit in terms of improved periodontal condition. In summary, AMY-101 appears to be a promising candidate drug for the adjunctive treatment of human periodontitis, a notion that merits investigation in human clinical trials.
| ln Vivo |
For NHPs with naturally occurring chronic periodontitis, AMY-101 can help with periodontal health [1]. Long-lasting anti-inflammatory effects can be produced by AMY-101 [1]. Subcutaneous administration of AMY-101 (4 mg/kg body weight, every 24 hours for 28 days) significantly and sustainably lowers PPD, a metric for tissue destruction [1]. In UUO-induced renal fibrosis, AMY-101 (Cp40, 1 mg/kg, subcutaneous injection every 12 hours, once daily for 7 or 14 days) decreases fibrosis and inflammatory cell infiltration [3].
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| Animal Protocol |
Animal/Disease Models: 15 adult male cynomolgus monkeys (Macaca fascicularis) (7-15 years old; weight 5.0-7.6 kg) [1].
Doses: 0.1 mg/site; 50 μL of 2 mg/mL solution. Route of Administration: local injection. (3 times a week or 1 time a week for 6 weeks, then 6 weeks of follow-up, no treatment required.) Experimental Results: No irritation to healthy gums. Animal/Disease Models: UUO and sham-operated mice [3]. Doses: 1 mg/kg. Route of Administration: Inject subcutaneously (sc) (sc) every 12 hrs (hrs (hours)) one time/day for 7 or 14 days. Experimental Results: 1 mg/kg Cp40 produced Dramatically less severe interstitial fibrosis than control mice injected with the peptide. |
| References |
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| Additional Infomation |
AMY-101, also known as compstatin 40, is a peptidic inhibitor of the central complement component C3. AMY-101 is under investigation in clinical trial NCT03694444 (A Study of the C3 Complement Inhibitor AMY-101 in Adults With Gingivitis).
C3 Complement Inhibitor AMY-101 is a compstatin-based inhibitor of human complement component C3, with potential use as a treatment for various diseases in which excessive complement activation plays a key role, including paroxysmal nocturnal hemoglobinuria (PNH) and complement 3 glomerulopathy (C3G). Upon administration, C3 complement inhibitor AMY-101 selectively binds to C3 and inhibits C3 activity. This prevents complement pathway activation, and inhibits complement-mediated inflammation and cell lysis. Excessive complement activation plays a key role in various inflammatory and autoimmune diseases, and leads to tissue destruction. C3 is a crucial and central component of the complement system, and the complement system is an integral component of the innate immune response. |
| Molecular Formula |
C83H117N23O18S2
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|---|---|
| Molecular Weight |
1789.09039473534
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| Exact Mass |
1787.838
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| CAS # |
1427001-89-5
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| Related CAS # |
AMY-101 TFA;1789738-04-0;AMY-101 acetate
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| PubChem CID |
131634231
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| Appearance |
White to off-white solid powder
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| LogP |
-2.1
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| Hydrogen Bond Donor Count |
21
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| Hydrogen Bond Acceptor Count |
23
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| Rotatable Bond Count |
30
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| Heavy Atom Count |
126
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| Complexity |
3770
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| Defined Atom Stereocenter Count |
15
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| SMILES |
CC[C@H](C)[C@@H](C(=O)N[C@H]1CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CN(C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC1=O)C(C)C)CC2=CN(C3=CC=CC=C32)C)CCC(=O)N)CC(=O)O)CC4=CNC5=CC=CC=C54)C)C)CC6=CN=CN6)CCCNC(=N)N)C(=O)N(C)[C@@H]([C@@H](C)CC)C(=O)N)NC(=O)[C@@H](CC7=CC=C(C=C7)O)N
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| InChi Key |
MUSGYEMSJUFFHT-UWABRSFTSA-N
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| InChi Code |
InChI=1S/C83H117N23O18S2/c1-11-43(5)68(103-72(114)53(84)30-46-23-25-50(107)26-24-46)80(122)100-61-39-125-126-40-62(82(124)106(10)69(70(86)112)44(6)12-2)101-73(115)55(21-17-29-90-83(87)88)94-76(118)58(33-49-36-89-41-92-49)96-71(113)45(7)93-65(109)38-105(9)81(123)60(31-47-35-91-54-20-15-13-18-51(47)54)99-77(119)59(34-66(110)111)97-74(116)56(27-28-64(85)108)95-75(117)57(98-79(121)67(42(3)4)102-78(61)120)32-48-37-104(8)63-22-16-14-19-52(48)63/h13-16,18-20,22-26,35-37,41-45,53,55-62,67-69,91,107H,11-12,17,21,27-34,38-40,84H2,1-10H3,(H2,85,108)(H2,86,112)(H,89,92)(H,93,109)(H,94,118)(H,95,117)(H,96,113)(H,97,116)(H,98,121)(H,99,119)(H,100,122)(H,101,115)(H,102,120)(H,103,114)(H,110,111)(H4,87,88,90)/t43-,44-,45-,53+,55-,56-,57-,58-,59-,60-,61-,62-,67-,68-,69-/m0/s1
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| Chemical Name |
2-((4R,7S,10S,13S,19S,22S,25S,28S,31S,34R)-10-((1H-imidazol-5-yl)methyl)-19-((1H-indol-3-yl)methyl)-34-((2S,3S)-2-((R)-2-amino-3-(4-hydroxyphenyl)propanamido)-3-methylpentanamido)-4-(((2S,3S)-1-amino-3-methyl-1-oxopentan-2-yl)(methyl)carbamoyl)-25-(3-amino-3-oxopropyl)-7-(3-guanidinopropyl)-31-isopropyl-13,17-dimethyl-28-((1-methyl-1H-indol-3-yl)methyl)-6,9,12,15,18,21,24,27,30,33-decaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32-decaazacyclopentatriacontan-22-yl)acetic acid
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| Synonyms |
AMY-101; AMY 101; AMY101;Compstatin 40; CP40; CP 40; CP-40;
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.5589 mL | 2.7947 mL | 5.5894 mL | |
| 5 mM | 0.1118 mL | 0.5589 mL | 1.1179 mL | |
| 10 mM | 0.0559 mL | 0.2795 mL | 0.5589 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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