| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
With an IC50 value of 95 μM, tcY-NH2 (0-500 μM) inhibits the aggregation of platelets (obtained from male albino Sprague-Dawley rats) induced by AYPGKF-NH2 (10 μM). With IC50 values of 64 μM for aorta relaxation (RA) and 1 μM for gastric contraction (LM), tcY-NH2 potently activates these processes[1]. Platelet aggregation caused by thrombin or AY-NH2 induces endostatin release, which is inhibited by tcY-NH2 (Tc-YPGKF-NH2, 400 μM, 5 min)[2]. In an isolated heart model, tcY-NH2 (5 μM, 15 min) increases recovery of ventricular function by 26% and decreases infarct size (IS) by 51%[5].
|
|---|---|
| ln Vivo |
In the Brain Death (BD) rat model, tcY-NH2 (tail vein injection, 0.6 mg/kg for a single dosage) reduces liver injury as seen by improved histomorphology and decreased blood ALT/AST levels[3]. In the draining lymph nodes of burn damage mice model, tcY-NH2 (intraperitoneal injection, 0.6 mg/kg for a single dosage) promotes posttraumatic activation of CD4+ Tregs[4]. In experimental inflammation in mice, tcY-NH2 (intrapleural injection, 40 ng/kg for a single dose) suppresses neutrophil recruitment[6].
|
| Animal Protocol |
Animal/Disease Models: Brain death (BD) rat model[3]
Doses: 0.6 mg/kg for a single dose Route of Administration: Tail vein injection for a single dose Experimental Results: decreased blood platelet activation and hepatic platelet accumulation. Attenuated the inflammatory response and apoptosis in the livers. Inhibited the activation of NF-κB and MAPK pathways induced by Brain death (BD). Animal/Disease Models: Burn injury model of C57BL/6 N mice[4] Doses: 0.6 mg/kg for a single dose Route of Administration: intraperitoneal (ip) injection Experimental Results: Increased expression and phosphorylation of PKC-θ in the presence of platelets, without affecting early posttraumatic hemostasis. Animal/Disease Models: BALB/c mice[6] Doses: 40 ng/kg for a single dose Route of Administration: Intrapleural injection Experimental Results: Abolished the number of rolling and adhering neutrophils on the vessel wall. Inhibited CXCL8- and Cg-induced neutrophil migration into the pleural cavity of mice. |
| References |
|
| Molecular Formula |
C40H49N7O7
|
|---|---|
| Molecular Weight |
739.86
|
| Exact Mass |
853.362
|
| CAS # |
327177-34-4
|
| Related CAS # |
tcY-NH2 TFA;1262750-73-1
|
| PubChem CID |
11479675
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
4.602
|
| Hydrogen Bond Donor Count |
7
|
| Hydrogen Bond Acceptor Count |
8
|
| Rotatable Bond Count |
19
|
| Heavy Atom Count |
54
|
| Complexity |
1270
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
O=C(NC(C(N1CCCC1C(NCC(NC(C(NC(C(N)=O)CC1C=CC=CC=1)=O)CCCCN)=O)=O)=O)CC1C=CC(O)=CC=1)/C=C/C1C=CC=CC=1
|
| InChi Key |
XKRAKQXQVIGYQC-PHOSSJRVSA-N
|
| InChi Code |
InChI=1S/C40H49N7O7/c41-22-8-7-14-31(38(52)46-32(37(42)51)24-28-12-5-2-6-13-28)44-36(50)26-43-39(53)34-15-9-23-47(34)40(54)33(25-29-16-19-30(48)20-17-29)45-35(49)21-18-27-10-3-1-4-11-27/h1-6,10-13,16-21,31-34,48H,7-9,14-15,22-26,41H2,(H2,42,51)(H,43,53)(H,44,50)(H,45,49)(H,46,52)/b21-18+/t31-,32-,33-,34-/m0/s1
|
| Chemical Name |
(2S)-N-[2-[[(2S)-6-amino-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-1-oxohexan-2-yl]amino]-2-oxoethyl]-1-[(2S)-3-(4-hydroxyphenyl)-2-[[(E)-3-phenylprop-2-enoyl]amino]propanoyl]pyrrolidine-2-carboxamide
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 1.3516 mL | 6.7580 mL | 13.5161 mL | |
| 5 mM | 0.2703 mL | 1.3516 mL | 2.7032 mL | |
| 10 mM | 0.1352 mL | 0.6758 mL | 1.3516 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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