WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H597585
CAS#: 93287-54-8
Description: Cgp 29287 is a primate-specific renin inhibitor with prolonged duration of action.
Hodoodo Cat#: H597585
Name: Cgp 29287
CAS#: 93287-54-8
Chemical Formula: C72H110N20O15
Exact Mass: 1,494.85
Molecular Weight: 1,495.790
Elemental Analysis: C, 57.81; H, 7.41; N, 18.73; O, 16.04
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Synonym: Cgp 29287; Cgp-29287; Cgp29287; Cgp-29,287; Cgp 29,287; Cgp29,287;
IUPAC/Chemical Name: methyl N2-((3S,4S)-4-((S)-2-((S)-2-((S)-1-(((benzyloxy)carbonyl)-L-arginyl-L-arginyl)pyrrolidine-2-carboxamido)-3-phenylpropanamido)-3-(1H-imidazol-4-yl)propanamido)-3-hydroxy-6-methylheptanoyl)-L-isoleucyl-L-histidyl-N6-(tert-butoxycarbonyl)-L-lysinate
InChi Key: DLAHCJHYEAZDLE-VRYQDWSQSA-N
InChi Code: InChI=1S/C72H110N20O15/c1-9-44(4)59(65(100)89-55(36-48-39-78-42-83-48)62(97)85-51(67(102)105-8)25-16-17-29-81-70(103)107-72(5,6)7)91-58(94)37-57(93)52(33-43(2)3)86-63(98)54(35-47-38-77-41-82-47)87-61(96)53(34-45-21-12-10-13-22-45)88-64(99)56-28-20-32-92(56)66(101)50(27-19-31-80-69(75)76)84-60(95)49(26-18-30-79-68(73)74)90-71(104)106-40-46-23-14-11-15-24-46/h10-15,21-24,38-39,41-44,49-57,59,93H,9,16-20,25-37,40H2,1-8H3,(H,77,82)(H,78,83)(H,81,103)(H,84,95)(H,85,97)(H,86,98)(H,87,96)(H,88,99)(H,89,100)(H,90,104)(H,91,94)(H4,73,74,79)(H4,75,76,80)/t44-,49-,50-,51-,52-,53-,54-,55-,56-,57-,59-/m0/s1
SMILES Code: O=C(OC)[C@H](CCCCNC(OC(C)(C)C)=O)NC([C@H](CC1=CNC=N1)NC([C@H]([C@@H](C)CC)NC(C[C@H](O)[C@@H](NC([C@H](CC2=CNC=N2)NC([C@H](CC3=CC=CC=C3)NC([C@H]4N(C([C@H](CCCNC(N)=N)NC([C@H](CCCNC(N)=N)NC(OCC5=CC=CC=C5)=O)=O)=O)CCC4)=O)=O)=O)CC(C)C)=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:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 1,495.79 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 |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Samani NJ, Cumin F, Kelly M, Wood JM. Expression of components of the RAS during prolonged blockade at different levels in primates. Am J Physiol. 1994 Oct;267(4 Pt 1):E612-9. PubMed PMID: 7943312.
2: Humke U, Levens N, Wood J, Hofbauer K. Responses to renin inhibition in conscious primates. Am J Physiol. 1991 Jul;261(1 Pt 2):F179-86. PubMed PMID: 1907105.
3: Nussberger J, Brunner DB, Waeber B, Brunner HR. In vitro renin inhibition to prevent generation of angiotensins during determination of angiotensin I and II. Life Sci. 1988;42(17):1683-8. PubMed PMID: 2835564.
4: de Gasparo MM, Wood JM, Heusser CH. Mechanism of inhibition of human renin by monoclonal antibodies. Hypertension. 1988 Mar;11(3):209-16. PubMed PMID: 3280480.
5: Wood JM, Jobber RA, Baum HP, Hofbauer KG. Comparison of chronic inhibition of renin and converting enzyme in the marmoset. Clin Exp Hypertens A. 1987;9(2-3):337-43. PubMed PMID: 3038392.
6: Wood JM, Baum HP, Carleton J, Dzau VJ. Inhibition of renin-like activity in marmoset tissues by the renin inhibitor CGP 29 287. J Hypertens Suppl. 1987 Jul;5(2):S67-9. PubMed PMID: 3116182.
7: Wood JM, Gulati N, Forgiarini P, Fuhrer W, Hofbauer KG. Effects of a specific and long-acting renin inhibitor in the marmoset. Hypertension. 1985 Sep-Oct;7(5):797-803. PubMed PMID: 3928488.
8: Wood JM, Baum HP, Forgiarini P, Gulati N, Jobber RA, Neisius D, Hofbauer KG. Haemodynamic effects of acute and chronic renin inhibition in marmosets. J Hypertens Suppl. 1989 Apr;7(2):S37-42. PubMed PMID: 2547039.
9: Wood JM, Baum HP, Jobber RA, Neisius D. Sustained reduction in blood pressure during chronic administration of a renin inhibitor to normotensive marmosets. J Cardiovasc Pharmacol. 1987;10 Suppl 7:S96-8. PubMed PMID: 2485073.
10: Wood JM, Jobber RA, Baum HP, de Gasparo M, Nussberger J. Biochemical effects of prolonged renin inhibition in marmosets. J Hypertens. 1989 Aug;7(8):615-8. PubMed PMID: 2681408.
11: Neisius D, Wood JM, Hofbauer KG. Renal vasodilatation after inhibition of renin or converting enzyme in marmoset. Am J Physiol. 1986 Nov;251(5 Pt 2):H897-902. PubMed PMID: 3022608.
12: Hofbauer KG, Fuhrer W, Heusser C, Wood JM. Comparison of different drug interference with the renin-angiotensin system. J Cardiovasc Pharmacol. 1985;7 Suppl 4:S62-8. PubMed PMID: 2412016.
13: Hofbauer KG, Wood JM, Gulati N, Heusser C, Ménard J. Increased plasma renin during renin inhibition. Studies with a novel immunoassay. Hypertension. 1985 May-Jun;7(3 Pt 2):I61-5. PubMed PMID: 2987126.
14: Neisius D, Wood JM. Antihypertensive effect of a renin inhibitor in marmosets with a segmental renal infarction. J Hypertens. 1987 Dec;5(6):721-5. PubMed PMID: 2828470.
15: Song K, Miyazaki M, Okunishi H, Ishii K, Takai S, Shiota N, Kim S, Mendelsohn FA. Localization and quantitation of active renin in monkey kidney by radioinhibitor binding and in vitro autoradiography. Am J Hypertens. 1994 Jun;7(6):529-35. PubMed PMID: 7917151.