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MedKoo Cat#: 597494 | Name: MEN 10376

Description:

WARNING: This product is for research use only, not for human or veterinary use.

MEN 10376 is a tachykinin receptor antagonist.

Chemical Structure

MEN 10376
MEN 10376
CAS#135306-85-3

Theoretical Analysis

MedKoo Cat#: 597494

Name: MEN 10376

CAS#: 135306-85-3

Chemical Formula: C57H68N12O10

Exact Mass: 1080.5181

Molecular Weight: 1081.24

Elemental Analysis: C, 63.32; H, 6.34; N, 15.55; O, 14.80

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
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Synonym
MEN 10376; MEN-10376; MEN10376; 5-Tyr-6,8,9-trp-10-lys-neurokinin A (4-10);
IUPAC/Chemical Name
(3S,6S,9R,12S,15R,18R,21S)-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-hexaazapentacosanoic acid
InChi Key
QQHOFZNACVKNHK-SXVLBCBNSA-N
InChi Code
InChI=1S/C57H68N12O10/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/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)/t40-,44-,45-,46+,47+,48+,50-/m0/s1
SMILES Code
NCCCC[C@@H](C(N)=O)NC([C@@H](CC1=CNC2=C1C=CC=C2)NC([C@@H](CC3=CNC4=C3C=CC=C4)NC([C@H](C(C)C)NC([C@@H](CC5=CNC6=C5C=CC=C6)NC([C@H](CC7=CC=C(O)C=C7)NC([C@H](CC(O)=O)N)=O)=O)=O)=O)=O)=O
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 1,081.24 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Quartara L, Patacchini R, Giuliani S, Renzetti AR, Rovero P, Maggi CA. N-terminal truncated analogs of men 10376 as tachykinin NK-2 receptor antagonists. Life Sci. 1992;51(25):1929-36. PubMed PMID: 1333561. 2: Bongianni F, Mutolo D, Cinelli E, Pantaleo T. Neurokinin receptor modulation of respiratory activity in the rabbit. Eur J Neurosci. 2008 Jun;27(12):3233-43. doi: 10.1111/j.1460-9568.2008.06295.x. Epub 2008 Jun 1. PubMed PMID: 18554294. 3: Venugopal CS, Christopher CL, Wilson SM, Polikepahad S, Dequeant E, Holmes EP. Pharmacologic evaluation of neurokinin-2 receptor antagonists in the guinea pig respiratory tract. Am J Vet Res. 2004 Jul;65(7):984-91. PubMed PMID: 15281659. 4: Maggi CA, Giuliani S, Ballati L, Lecci A, Manzini S, Patacchini R, Renzetti AR, Rovero P, Quartara L, Giachetti A. 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. PubMed PMID: 1710662. 5: Astolfi M, Treggiari S, Giachetti A, Meini S, Maggi CA, Manzini S. Characterization of the tachykinin NK2 receptor in the human bronchus: influence of amastatin-sensitive metabolic pathways. Br J Pharmacol. 1994 Feb;111(2):570-4. PubMed PMID: 8004400; PubMed Central PMCID: PMC1909962. 6: Johansson A, Liu L, Holmgren S, Burcher E. Characterization of receptors for two Xenopus gastrointestinal tachykinin peptides in their species of origin. Naunyn Schmiedebergs Arch Pharmacol. 2004 Jul;370(1):35-45. Epub 2004 Jul 2. PubMed PMID: 15235762. 7: Mutolo D, Bongianni F, Cinelli E, Pantaleo T. Depression of cough reflex by microinjections of antitussive agents into caudal ventral respiratory group of the rabbit. J Appl Physiol (1985). 2010 Oct;109(4):1002-10. doi: 10.1152/japplphysiol.00406.2010. Epub 2010 Jul 22. PubMed PMID: 20651222. 8: Liu H, Miller DV, Lourenssen S, Wells RW, Blennerhassett MG, Paterson WG. Proteinase-activated receptor-2 activation evokes oesophageal longitudinal smooth muscle contraction via a capsaicin-sensitive and neurokinin-2 receptor-dependent pathway. Neurogastroenterol Motil. 2010 Feb;22(2):210-6, e67. doi: 10.1111/j.1365-2982.2009.01394.x. Epub 2009 Sep 9. PubMed PMID: 19740117. 9: Smits GJ, Lefebvre RA. Tachykinin receptors involved in the contractile effect of the natural tachykinins in the rat gastric fundus. J Auton Pharmacol. 1994 Dec;14(6):383-92. PubMed PMID: 7533168. 10: Luo L, Wiesenfeld-Hallin Z. The effects of pretreatment with tachykinin antagonists and galanin on the development of spinal cord hyperexcitability following sciatic nerve section in the rat. Neuropeptides. 1995 Mar;28(3):161-6. PubMed PMID: 7540733. 11: Mutolo D, Bongianni F, Cinelli E, Fontana GA, Pantaleo T. Modulation of the cough reflex by antitussive agents within the caudal aspect of the nucleus tractus solitarii in the rabbit. Am J Physiol Regul Integr Comp Physiol. 2008 Jul;295(1):R243-51. doi: 10.1152/ajpregu.00184.2008. Epub 2008 May 14. PubMed PMID: 18480245. 12: Renzetti LM, Shenvi A, Buckner CK. Nonadrenergic, noncholinergic contractile responses of the guinea pig hilar bronchus involve the preferential activation of tachykinin neurokinin2 receptors. J Pharmacol Exp Ther. 1992 Sep;262(3):957-63. PubMed PMID: 1326630. 13: Kemény LV, Hegyi P, Rakonczay Z Jr, Borka K, Korompay A, Gray MA, Argent BE, Venglovecz V. Substance P inhibits pancreatic ductal bicarbonate secretion via neurokinin receptors 2 and 3 in the guinea pig exocrine pancreas. Pancreas. 2011 Jul;40(5):793-5. doi: 10.1097/MPA.0b013e3182161d05. PubMed PMID: 21673544. 14: Maggi CA, Patacchini R, Eglezos A, Quartara L, Giuliani S, Giachetti A. Tachykinin receptors in the guinea-pig renal pelvis: activation by exogenous and endogenous tachykinins. Br J Pharmacol. 1992 Sep;107(1):27-33. PubMed PMID: 1384907; PubMed Central PMCID: PMC1907585. 15: Ellis JL, Undem BJ. Antigen-induced enhancement of noncholinergic contractile responses to vagus nerve and electrical field stimulation in guinea pig isolated trachea. J Pharmacol Exp Ther. 1992 Aug;262(2):646-53. PubMed PMID: 1323657. 16: Tan-No K, Esashi A, Nakagawasai O, Niijima F, Tadano T, Sakurada C, Sakurada T, Bakalkin G, Terenius L, Kisara K. Intrathecally administered big dynorphin, a prodynorphin-derived peptide, produces nociceptive behavior through an N-methyl-D-aspartate receptor mechanism. Brain Res. 2002 Oct 11;952(1):7-14. PubMed PMID: 12363399. 17: Russo RE, Nagy F, Hounsgaard J. Modulation of plateau properties in dorsal horn neurones in a slice preparation of the turtle spinal cord. J Physiol. 1997 Mar 1;499 ( Pt 2):459-74. PubMed PMID: 9080374; PubMed Central PMCID: PMC1159319. 18: Patacchini R, Quartara L, Rovero P, Goso C, Maggi CA. Role of C-terminal amidation on the biological activity of neurokinin A derivatives with agonist and antagonist properties. J Pharmacol Exp Ther. 1993 Jan;264(1):17-21. PubMed PMID: 8380857. 19: Wiesenfeld-Hallin Z, Luo L, Xu XJ, Maggi CA. Differential effects of selective tachykinin NK2 receptor antagonists in rat spinal cord. Eur J Pharmacol. 1994 Jan 4;251(1):99-102. PubMed PMID: 8137876. 20: Bartho L, Santicioli P, Patacchini R, Maggi CA. Tachykininergic transmission to the circular muscle of the guinea-pig ileum: evidence for the involvement of NK2 receptors. Br J Pharmacol. 1992 Apr;105(4):805-10. PubMed PMID: 1380373; PubMed Central PMCID: PMC1908693.

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