1. GPCR/G Protein Neuronal Signaling
  2. Adrenergic Receptor
  3. (S)-Terazosin

(S)-Terazosin is an active S-enantiomer of Terazosin. (S)-Terazosin is a potent and high-affinity α-adrenoceptor antagonist with Ki values of 3.91 nM, 0.79 nM and 1.16 nM for α1a, α1b and α1d-adrenoceptor, respectively. (S)-Terazosin also has high-affinity for α2a, α2B and α2c-adrenoceptor with Ki values of 729 nM, 3.5 nM and 46.4 nM, respectively.

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(S)-Terazosin Chemical Structure

(S)-Terazosin Chemical Structure

CAS No. : 109351-33-9

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Based on 1 publication(s) in Google Scholar

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Description

(S)-Terazosin is an active S-enantiomer of Terazosin. (S)-Terazosin is a potent and high-affinity α-adrenoceptor antagonist with Ki values of 3.91 nM, 0.79 nM and 1.16 nM for α1a, α1b and α1d-adrenoceptor, respectively. (S)-Terazosin also has high-affinity for α2a, α2B and α2c-adrenoceptor with Ki values of 729 nM, 3.5 nM and 46.4 nM, respectively[1].

IC50 & Target

Ki: 3.91 nM (α1a-adrenoceptor), 0.79 nM (α1b-adrenoceptor) and 1.16 nM (α1d-adrenoceptor); 729 nM (α2a-adrenoceptor), 3.5 nM (α2Ba-adrenoceptor) and 46.4 nM (α2c-adrenoceptor)[1]

In Vitro

The racemic compound and its enantiomers show high and apparently equal affinity for subtypes of α1-adrenoceptors with Ki values in the low nanomolar range, and showed potent antagonism of α1-adrenoceptors in isolated tissues, with the enantiomers approximately equipotent to the racemate at each α1-adrenoceptor subtype. At α2b sites, (R)-Terazosin binds less potently than either the (S)-Terazosin or racemate[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

(S)-Terazosin shows antagonism of at rat atrial α2B receptor with a pEC30 of 6.93. (s)-Terazosin shows antagonism of at rat vas deferens α1A and α2A receptor with pA2 values of 8.3 and 6.12, respectively[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

387.43

Formula

C19H25N5O4

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCN(C2=NC(N)=C3C=C(OC)C(OC)=CC3=N2)CC1)[C@H]4OCCC4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 150 mg/mL (387.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5811 mL 12.9056 mL 25.8111 mL
5 mM 0.5162 mL 2.5811 mL 5.1622 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Purity & Documentation
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Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5811 mL 12.9056 mL 25.8111 mL 64.5278 mL
5 mM 0.5162 mL 2.5811 mL 5.1622 mL 12.9056 mL
10 mM 0.2581 mL 1.2906 mL 2.5811 mL 6.4528 mL
15 mM 0.1721 mL 0.8604 mL 1.7207 mL 4.3019 mL
20 mM 0.1291 mL 0.6453 mL 1.2906 mL 3.2264 mL
25 mM 0.1032 mL 0.5162 mL 1.0324 mL 2.5811 mL
30 mM 0.0860 mL 0.4302 mL 0.8604 mL 2.1509 mL
40 mM 0.0645 mL 0.3226 mL 0.6453 mL 1.6132 mL
50 mM 0.0516 mL 0.2581 mL 0.5162 mL 1.2906 mL
60 mM 0.0430 mL 0.2151 mL 0.4302 mL 1.0755 mL
80 mM 0.0323 mL 0.1613 mL 0.3226 mL 0.8066 mL
100 mM 0.0258 mL 0.1291 mL 0.2581 mL 0.6453 mL
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(S)-Terazosin Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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(S)-Terazosin
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