Synonym
TAK-637, TAK 637, TAK637
IUPAC/Chemical Name
(9R)-7-[[3,5-bis(trifluoromethyl)phenyl]methyl]-9-methyl-5-(4-methylphenyl)-8,9,10,11-tetrahydro-[1,4]diazocino[2,1-g][1,7]naphthyridine-6,13-dione
InChi Key
LDXQLWNPGRANTO-GOSISDBHSA-N
InChi Code
InChI=1S/C30H25F6N3O2/c1-17-5-7-20(8-6-17)24-23-4-3-10-37-25(23)27(40)39-11-9-18(2)15-38(28(41)26(24)39)16-19-12-21(29(31,32)33)14-22(13-19)30(34,35)36/h3-8,10,12-14,18H,9,11,15-16H2,1-2H3/t18-/m1/s1
SMILES Code
O=C1N(CC2=CC(C(F)(F)F)=CC(C(F)(F)F)=C2)C[C@H](C)CCN3C1=C(C4=CC=C(C)C=C4)C5=C(N=CC=C5)C3=O
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
>2 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
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
573.54
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.
| 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: Tarui N, Ikeura Y, Natsugari H, Nakahama K. Microbial synthesis of three metabolites of a tachykinin receptor antagonist, TAK-637. J Biosci Bioeng. 2001;92(3):285-7. PubMed PMID: 16233097.
2: Venkova K, Greenwood-Van Meerveld B. Effects of TAK-637 on NK(1) receptor-mediated mechanisms regulating colonic secretion. Toxicol Appl Pharmacol. 2004 Apr 15;196(2):215-22. PubMed PMID: 15081268.
3: Furness JB. TAK-637. Takeda. Curr Opin Investig Drugs. 2001 Oct;2(10):1437-40. Review. PubMed PMID: 11890361.
4: Venkova K, Sutkowski-Markmann DM, Greenwood-Van Meerveld B. Peripheral activity of a new NK1 receptor antagonist TAK-637 in the gastrointestinal tract. J Pharmacol Exp Ther. 2002 Mar;300(3):1046-52. PubMed PMID: 11861814.
5: Kamo I, Doi T. Effect of TAK-637, a tachykinin NK1-receptor antagonist, on lower urinary tract function in cats. Jpn J Pharmacol. 2001 Jun;86(2):165-9. PubMed PMID: 11459118.
6: Okano S, Nagaya H, Ikeura Y, Natsugari H, Inatomi N. Effects of TAK-637, a novel neurokinin-1 receptor antagonist, on colonic function in vivo. J Pharmacol Exp Ther. 2001 Aug;298(2):559-64. PubMed PMID: 11454917.
7: Kamo I, Imai S, Okanishi S, Doi T. Possible site of action of TAK-637, a tachykinin NK(1) receptor antagonist, on the micturition reflex in guinea pigs. Eur J Pharmacol. 2000 Aug 4;401(2):235-40. PubMed PMID: 10924932.
8: Doi T, Kamo I, Imai S, Okanishi S, Ikeura Y, Natsugari H. Effects of TAK-637, a tachykinin receptor antagonist, on the micturition reflex in guinea pigs. Eur J Pharmacol. 2000 May 3;395(3):241-6. PubMed PMID: 10812055.
9: Doi T, Kamo I, Imai S, Okanishi S, Ishimaru T, Ikeura Y, Natsugari H. Effects of TAK-637, a tachykinin receptor antagonist, on lower urinary tract function in the guinea pig. Eur J Pharmacol. 1999 Nov 3;383(3):297-303. PubMed PMID: 10594323.
