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Temocapril HCl

CAS# 110221-44-8

Temocapril HCl

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Chemical structure

Temocapril HCl

3D structure

Chemical Properties of Temocapril HCl

Cas No. 110221-44-8 SDF Download SDF
PubChem ID 443873 Appearance Powder
Formula C23H29ClN2O5S2 M.Wt 513.07
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : ≥ 100 mg/mL (194.91 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 2-[(2S,6R)-6-[[(2S)-1-ethoxy-1-oxo-4-phenylbutan-2-yl]amino]-5-oxo-2-thiophen-2-yl-1,4-thiazepan-4-yl]acetic acid;hydrochloride
SMILES CCOC(=O)C(CCC1=CC=CC=C1)NC2CSC(CN(C2=O)CC(=O)O)C3=CC=CS3.Cl
Standard InChIKey XDDQNOKKZKHBIX-ASBZXGSUSA-N
Standard InChI InChI=1S/C23H28N2O5S2.ClH/c1-2-30-23(29)17(11-10-16-7-4-3-5-8-16)24-18-15-32-20(19-9-6-12-31-19)13-25(22(18)28)14-21(26)27;/h3-9,12,17-18,20,24H,2,10-11,13-15H2,1H3,(H,26,27);1H/t17-,18-,20-;/m0./s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Temocapril HCl

DescriptionTemocapril Hydrochloride is a long-acting angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension. Target: ACE Temocapril hydrochloride is a novel prodrug-type angiotensin-I converting enzyme (ACE) inhibitor, lowering of the dose of temocapril might be recommended only in patients with severe renal insufficiency [1]. Temocapril is regarded as an ACE inhibitor the disposition and efficacy of which are little affected in patients with impaired liver function [2].

References:
[1]. Nakashima, M., et al., Pharmacokinetics of temocapril hydrochloride, a novel angiotensin converting enzyme inhibitor, in renal insufficiency. Eur J Clin Pharmacol, 1992. 43(6): p. 657-9. [2]. Furuta, S., et al., Pharmacokinetics of temocapril, an ACE inhibitor with preferential biliary excretion, in patients with impaired liver function. Eur J Clin Pharmacol, 1993. 44(4): p. 383-5.

Temocapril HCl Dilution Calculator

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Temocapril HCl Molarity Calculator

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Preparing Stock Solutions of Temocapril HCl

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 1.9491 mL 9.7453 mL 19.4905 mL 38.981 mL 48.7263 mL
5 mM 0.3898 mL 1.9491 mL 3.8981 mL 7.7962 mL 9.7453 mL
10 mM 0.1949 mL 0.9745 mL 1.9491 mL 3.8981 mL 4.8726 mL
50 mM 0.039 mL 0.1949 mL 0.3898 mL 0.7796 mL 0.9745 mL
100 mM 0.0195 mL 0.0975 mL 0.1949 mL 0.3898 mL 0.4873 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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References on Temocapril HCl

Study on pharmacokinetics of a new biliary excreted oral angiotensin converting enzyme inhibitor, temocapril (CS-622) in humans.[Pubmed:8427943]

Biopharm Drug Dispos. 1993 Jan;14(1):41-50.

Despite the usefulness of angiotensin converting enzyme (ACE; EC 3.4.15.1) inhibitors for patients with renal insufficiency, some hesitation has been exercised in applying ACE inhibitors to the treatment of such patients because most ACE inhibitors are excreted mainly into the urine. In this context, development of an ACE inhibitor which is excreted into the bile has been sought. The pharmacokinetic properties of the novel ACE inhibitor, temocapril hydrochloride (Temocapril HCl; CS-622), were investigated in six healthy volunteers. This drug is excreted mainly into the bile in animal studies. Temocapril HCl was given in a single dose of 0.5, 1.0, and 2.0 mg, and 36, 44, and 38 per cent of the administered drug was excreted in the feces and 17, 19, and 24 per cent in the urine as the de-esterified active diacid form (the diacid metabolite) within 48 h, respectively. The plasma ACE activity was markedly inhibited. No abnormal clinical findings suggestive of side-effects were observed. Thus, from the pharmacokinetic standpoint, Temocapril HCl is expected to be a useful drug for patients with renal dysfunction.

Description

Temocapril Hydrochloride is a long-acting angiotensin-converting enzyme (ACE) inhibitor, used for the treatment of hypertension.

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