For research use only. Not for therapeutic Use.
Men 10376 TFA is a selective tachykinin NK-2 receptor antagonist, with a Ki of 4.4 μM for rat small intestine NK-2 receptor[1].
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].
| Catalog Number | I046222 |
| Synonyms | (3S)-3-amino-4-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2R)-1-[[(2R)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-4-oxobutanoic acid;2,2,2-trifluoroacetic acid |
| Molecular Formula | C59H69F3N12O12 |
| Purity | ≥95% |
| InChI | InChI=1S/C57H68N12O10.C2HF3O2/c1-31(2)50(69-56(78)48(26-35-30-63-43-16-8-5-13-39(35)43)67-53(75)45(23-32-18-20-36(70)21-19-32)65-52(74)40(59)27-49(71)72)57(79)68-47(25-34-29-62-42-15-7-4-12-38(34)42)55(77)66-46(24-33-28-61-41-14-6-3-11-37(33)41)54(76)64-44(51(60)73)17-9-10-22-58;3-2(4,5)1(6)7/h3-8,11-16,18-21,28-31,40,44-48,50,61-63,70H,9-10,17,22-27,58-59H2,1-2H3,(H2,60,73)(H,64,76)(H,65,74)(H,66,77)(H,67,75)(H,68,79)(H,69,78)(H,71,72);(H,6,7)/t40-,44-,45-,46+,47+,48+,50-;/m0./s1 |
| InChIKey | VVLJOWMNHFTRHU-UAZFYXPJSA-N |
| SMILES | CC(C)C(C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NC(CC3=CNC4=CC=CC=C43)C(=O)NC(CCCCN)C(=O)N)NC(=O)C(CC5=CNC6=CC=CC=C65)NC(=O)C(CC7=CC=C(C=C7)O)NC(=O)C(CC(=O)O)N.C(=O)(C(F)(F)F)O |
| Reference | [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. |
