MEN 10376 (Synonyms: DYWVWWK-NH2, Asp-Tyr-Trp-Val-Trp-Trp-Lys-NH2) |
| Katalog-Nr.GC17547 |
Men 10376 ist ein selektiver Tachykinin-NK-2-Rezeptorantagonist mit einem Ki von 4,4 μM fÜr den Ratten-DÜnndarm-NK-2-Rezeptor.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 135306-85-3
Sample solution is provided at 25 µL, 10mM.
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Men 10376 is a selective tachykinin NK-2 receptor antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor.
Men 10376 is a selective tachykinin NK-2 receptor, with a Ki of 4.4 μM, and shows low selectivity for NK-1 and NK-3 receptors (Ki, >10 μM)[1]. Men 10376 shows pA2s of 5.66 and 8.08 for NK-1 (guinea-pig ileum) and NK-2 receptors (endothelium-deprived rabbit pulmonary artery). Men 10376 shows no effect on NK-3 receptor (Ki, >10 μM)[2].
Men 10376 (1 and 3 μmol/kg) antagonizes increase in bladder motility produced by the NK-2 receptor agonist in rats[2].
References:
[1]. Quartara L, et al. N-terminal truncated analogs of men 10376 as tachykinin NK-2 receptor antagonists. Life Sci. 1992;51(25):1929-36.
[2]. Maggi CA, et al. In vivo evidence for tachykininergic transmission using a new NK-2 receptor-selective antagonist, MEN 10,376. J Pharmacol Exp Ther. 1991 Jun;257(3):1172-8.
| Cas No. | 135306-85-3 | SDF | |
| Überlieferungen | DYWVWWK-NH2, Asp-Tyr-Trp-Val-Trp-Trp-Lys-NH2 | ||
| Chemical Name | (3S,6S,9R,12R,15S,18S,21R)-9,15,18-tris((1H-indol-3-yl)methyl)-3,25-diamino-21-carbamoyl-6-(4-hydroxybenzyl)-12-isopropyl-4,7,10,13,16,19-hexaoxo-5,8,11,14,17,20-hexaazapentacosan-1-oic acid | ||
| Canonical SMILES | O=C([C@@H](C(C)C)NC([C@@H](CC1=CNC2=CC=CC=C12)NC([C@H](CC(C=C3)=CC=C3O)NC([C@H](CC(O)=O)N)=O)=O)=O)N[C@H](C(N[C@H](C(N[C@@H](C(N)=O)CCCCN)=O)CC4=CNC5=CC=CC=C45)=O)CC6=CNC7=CC=CC=C67 | ||
| Formula | C57H68N12O10 | M.Wt | 1081.24 |
| Löslichkeit | Water : 1.43 mg/mL (1.20 mM) | Storage | Desiccate at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.9249 mL | 4.6243 mL | 9.2486 mL |
| 5 mM | 0.185 mL | 0.9249 mL | 1.8497 mL |
| 10 mM | 0.0925 mL | 0.4624 mL | 0.9249 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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