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Temocaprilat

Catalog No. T20689   CAS 110221-53-9
Synonyms: RNH-5139, RS-5139, RNH 5139, RNH5139, RS5139, RS 5139

Temocaprilat (RS5139) is an Angiotensin-converting Enzyme (ACE) inhibitor. Temocaprilat is effectively excreted in bile via cMOAT that is deficient in EHBR and that many of other ACE inhibitors have low affinity for cMOAT.

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Temocaprilat Chemical Structure
Temocaprilat, CAS 110221-53-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 343.00
2 mg In stock $ 476.00
5 mg In stock $ 698.00
10 mg In stock $ 997.00
25 mg In stock $ 1,480.00
50 mg In stock $ 1,990.00
100 mg In stock $ 2,690.00
1 mL * 10 mM (in DMSO) In stock $ 836.00
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Purity: 96.88%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Temocaprilat (RS5139) is an Angiotensin-converting Enzyme (ACE) inhibitor. Temocaprilat is effectively excreted in bile via cMOAT that is deficient in EHBR and that many of other ACE inhibitors have low affinity for cMOAT.
In vivo Biliary clearance of Temocaprilat after i.v. administration of [14C]temocapril x HCl (1.0 mg/kg) in EHBR was significantly lower than that in Sprague-Dawley rats (5.00 ml/min/kg for Sprague-Dawley rats vs. 0.25 ml/min/kg for EHBR). The uptake of Temocaprilat into canalicular membrane vesicles (CMVs) prepared from Sprague-Dawley rats was stimulated in the presence of ATP, whereas little stimulation was observed in CMVs from EHBR. The initial uptake rate of ATP-dependent transport of Temocaprilat showed saturation kinetics; we obtained an apparent V(max) value of 1.14 nmol/min/mg protein and a K(m) value 92.5 microM. ATP-dependent transport of Temocaprilat was competitively inhibited by 2,4-dinitrophenyl-S-glutathione, a typical substrate for cMOAT with an inhibition constant (K(i)) of 25.8 microM. The K(m) value for the uptake of 2,4-dinitrophenyl-S-glutathione into CMVs (K(m) = 29.6 microM) was consistent with this K(i) value. In addition, the ATP-dependent uptake of 2,4-dinitrophenyl-S-glutathione was inhibited by Temocaprilat in a concentration-dependent manner. Active forms of some ACE inhibitors (benazepril, cilazapril, delapril, enalapril and imidapril) did not affect the transport of Temocaprilat into CMVs even at concentrations as high as 200 microM[1].
Synonyms RNH-5139, RS-5139, RNH 5139, RNH5139, RS5139, RS 5139
Molecular Weight 448.56
Formula C21H24N2O5S2
CAS No. 110221-53-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 4.49 mg/mL (10 mM)

TargetMolReferences and Literature

1. Ishizuka H, et al. Temocaprilat, a novel angiotensin-converting enzyme inhibitor, is excreted in bile via an ATP-dependent active transporter (cMOAT) that is deficient in Eisai hyperbilirubinemic mutant rats (EHBR). J Pharmacol Exp Ther. 1997 Mar;280(3):1304-11. 2. Yasunari K, et al. Converting enzyme inhibitor temocaprilat prevents high glucose-mediated suppression of human aortic endothelial cell proliferation. J Cardiovasc Pharmacol. 2003 Dec;42 Suppl 1:S55-60. 3. Püchler K, et al. Pharmacokinetics of temocapril and temocaprilat after 14 once daily oral doses of temocapril in hypertensive patients with varying degrees of renal impairment. Br J Clin Pharmacol. 1997 Dec;44(6):531-6. 4. Ishizuka H, et al. Transport of temocaprilat into rat hepatocytes: role of organic anion transporting polypeptide. J Pharmacol Exp Ther. 1998 Oct;287(1):37-42.

Related compound libraries

This product is contained In the following compound libraries:
Human Metabolite Library Bioactive Compounds Library Max Inhibitor Library Bioactive Compound Library Metabolism Compound Library

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Keywords

Temocaprilat 110221-53-9 Metabolism Angiotensin-converting Enzyme (ACE) RNH-5139 RS-5139 RNH 5139 RNH5139 RS5139 RS 5139 inhibitor inhibit

 

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