Synonym
NPC 17761; NPC17761; NPC-17761
IUPAC/Chemical Name
(1-(1-((1-(arginylarginylprolyl)-4-hydroxypyrrolidine-2-carbonyl)glycylphenylalanylseryl)-4-(phenylthio)pyrrolidine-2-carbonyl)octahydro-1H-indole-2-carbonyl)arginine
InChi Key
TTZWORQGJCRWCJ-UHFFFAOYSA-N
InChi Code
InChI=1S/C62H93N19O13S/c63-40(18-9-23-70-60(64)65)51(85)75-41(19-10-24-71-61(66)67)55(89)78-26-12-22-46(78)57(91)79-32-37(83)29-47(79)53(87)73-31-50(84)74-43(27-35-13-3-1-4-14-35)52(86)77-44(34-82)56(90)80-33-39(95-38-16-5-2-6-17-38)30-49(80)58(92)81-45-21-8-7-15-36(45)28-48(81)54(88)76-42(59(93)94)20-11-25-72-62(68)69/h1-6,13-14,16-17,36-37,39-49,82-83H,7-12,15,18-34,63H2,(H,73,87)(H,74,84)(H,75,85)(H,76,88)(H,77,86)(H,93,94)(H4,64,65,70)(H4,66,67,71)(H4,68,69,72)
SMILES Code
NC(C(NC(C(N1CCCC1C(N2CC(CC2C(NCC(NC(C(NC(C(N3CC(Sc4ccccc4)CC3C(N5C6CCCCC6CC5C(NC(C(O)=O)CCCNC(N)=N)=O)=O)=O)CO)=O)Cc7ccccc7)=O)=O)O)=O)=O)CCCNC(N)=N)=O)CCCNC(N)=N
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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
1,344.61
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: Otterbein L, Lowe VC, Kyle DJ, Noronha-Blob L. Additive effects of a bradykinin antagonist, NPC 17761, and a leumedin, NPC 15669, on survival in animal models of sepsis. Agents Actions. 1993;39 Spec No:C125-7. doi: 10.1007/BF01972742. PMID: 8273550.
2: Corrêa CR, Calixto JB. Evidence for participation of B1 and B2 kinin receptors in formalin-induced nociceptive response in the mouse. Br J Pharmacol. 1993 Sep;110(1):193-8. doi: 10.1111/j.1476-5381.1993.tb13791.x. PMID: 8220879; PMCID: PMC2176006.
3: Da Silva A, Amrani Y, Trifilieff A, Landry Y. Involvement of B2 receptors in the bradykinin-induced relaxation of guinea-pig isolated trachea. Br J Pharmacol. 1995 Jan;114(1):103-8. doi: 10.1111/j.1476-5381.1995.tb14912.x. PMID: 7712004; PMCID: PMC1510188.
4: Schlemper V, Calixto JB. Mechanisms involved in the relaxant response of bradykinin in epithelium intact strips of the guinea-pig trachea. Eur J Pharmacol. 1995 Aug 25;282(1-3):177-84. doi: 10.1016/0014-2999(95)00329-j. PMID: 7498273.
5: Dear JW, Wirth K, Scadding GK, Foreman JC. Characterization of the bradykinin receptor in the human nasal airway using the binding of [125I]-Hoe 140. Br J Pharmacol. 1996 Nov;119(5):1054-62. doi: 10.1111/j.1476-5381.1996.tb15777.x. PMID: 8922758; PMCID: PMC1915934.
6: Forteza R, Lauredo IT, Burch R, Abraham WM. Extracellular metabolites of Pseudomonas aeruginosa produce bronchoconstriction by different mechanisms. Am J Respir Crit Care Med. 1994 Mar;149(3 Pt 1):687-93. doi: 10.1164/ajrccm.149.3.8118638. PMID: 8118638.
7: Cabrini DA, Calixto JB. Characterization of des-Arg9-bradykinin-induced contraction in guinea-pig gallbladder in vitro. Eur J Pharmacol. 1997 Jul 16;331(1):31-8. doi: 10.1016/s0014-2999(97)01010-8. PMID: 9274927.
8: Trifilieff A, Amrani Y, Landry Y, Gies JP. Comparative action of new highly potent bradykinin receptor antagonists in the guinea-pig trachea. Eur J Pharmacol. 1993 Aug 3;239(1-3):227-9. doi: 10.1016/0014-2999(93)91000-d. PMID: 8223898.
9: Novotny EA, Bednar DL, Connolly MA, Connor JR, Stormann TM. Mutation of aspartate residues in the third extracellular loop of the rat B2 bradykinin receptor decreases affinity for bradykinin. Biochem Biophys Res Commun. 1994 Jun 15;201(2):523-30. doi: 10.1006/bbrc.1994.1733. PMID: 8002982.
10: Lach E, Trifilieff A, Mousli M, Landry Y, Gies JP. Bradykinin-induced contraction of guinea pig lung in vitro. Naunyn Schmiedebergs Arch Pharmacol. 1994 Aug;350(2):201-8. doi: 10.1007/BF00241097. PMID: 7990978.
