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

(R)-Terazosin 

Cat. No.: HY-B0371B Purity: 99.77% ee.: 100.00%
Handling Instructions

(R)-Terazosin is an active R-enantiomer of Terazosin. (R)-Terazosin is a potent α1-adrenoceptor antagonist with Ki values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively.

For research use only. We do not sell to patients.

(R)-Terazosin Chemical Structure

(R)-Terazosin Chemical Structure

CAS No. : 109351-34-0

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10 mM * 1  mL in DMSO USD 275 In-stock
Estimated Time of Arrival: December 31
5 mg USD 250 In-stock
Estimated Time of Arrival: December 31
10 mg USD 350 In-stock
Estimated Time of Arrival: December 31
50 mg USD 950 In-stock
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100 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

(R)-Terazosin is an active R-enantiomer of Terazosin. (R)-Terazosin is a potent α1-adrenoceptor antagonist with Ki values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively[1].

IC50 & Target

Ki: 6.51 nM (α1a-adrenoceptor), 1.01 nM (α1b-adrenoceptor) and 1.97 nM (α1d-adrenoceptor)[1]

In Vitro

(R)-Terazosin is low affinity for α2a, α2B and α2c-adrenoceptor with Ki values of 3.85 μM, 0.33 μM and 0.37 μM, respectively[1].
(R)-Terazosin may prove to be a useful probe in understanding the functional role of subtypes of adrenoceptors in various tissues. Because it is a weaker antagonist at α2B sites than its enantiomer, it may be possible to use (R)-Terazosin to differentiate between pharmacological effects mediated by subtypes of α2-adrenoceptors in animal studies[1].

In Vivo

(R)-Terazosin shows antagonism of at rat atrial α2B receptor with a pEC30 of 5.69. (R)-Terazosin shows antagonism of at rat vas deferens α1A and α2A receptor with pA2 values of 7.5 and 5.31, respectively[1].

Molecular Weight

387.43

Formula

C₁₉H₂₅N₅O₄

CAS No.

109351-34-0

SMILES

O=C(N1CCN(C2=NC(N)=C3C=C(OC)C(OC)=CC3=N2)CC1)[[email protected]@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 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 75 mg/mL (193.58 mM; Need ultrasonic)

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
10 mM 0.2581 mL 1.2906 mL 2.5811 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 7.5 mg/mL (19.36 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 7.5 mg/mL (19.36 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 7.5 mg/mL (19.36 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

(R)-TerazosinAdrenergic ReceptorBeta ReceptorLowaffinitysubtypesproveα2-adrenoceptorα1-adrenoceptorInhibitorinhibitorinhibit

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(R)-Terazosin
Cat. No.:
HY-B0371B
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