1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
    Autophagy
  2. Histamine Receptor
    Autophagy
  3. Clemastine fumarate

Clemastine fumarate (Synonyms: HS-592 fumarate; Meclastine fumarate)

Cat. No.: HY-B0298A Purity: 99.95%
Handling Instructions

Clemastine (fumarate) (HS-592 (fumarate)) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.

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

Clemastine fumarate Chemical Structure

Clemastine fumarate Chemical Structure

CAS No. : 14976-57-9

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
100 mg USD 60 In-stock
Estimated Time of Arrival: December 31
200 mg USD 96 In-stock
Estimated Time of Arrival: December 31
500 mg USD 197 In-stock
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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

Clemastine (fumarate) (HS-592 (fumarate)) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.

IC50 & Target

Histamine H1 Receptor[1].

In Vitro

Clemastine (fumarate) (HS-592 (fumarate)) inhibits histamine induced rise in [Ca2+]i in HL-60 cells with an IC50 of 3 nM as compared with that of chlorpheniramine or diphenhydramine with IC50 values of 20 nM and 100 nM, respectively[1]. Clemastine showed a first-pass reduction in the extent of absorption, with oral bioavailability calculated as 39.2 +/- 12.4%. Extravascular distribution of drug was suggested by the high volume of distribution (799 +/- 315 L) and low Cmax (0.577 +/- 0.252 ng/mL/mg) observed at 4.77 +/- 2.26 hours after administration, and by the biphasic decline in plasma concentration. The terminal elimination half-life (t1/2) of clemastine was 21.3 +/- 11.6 hours. Steady-state concentrations of clemastine were consistent with linear pharmacokinetic processes, and clearance was unaffected by age in the range studied, or by race[2].

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

Clinical Trial
Molecular Weight

459.96

Formula

C₂₅H₃₀ClNO₅

CAS No.

14976-57-9

SMILES

CN1[[email protected]@H](CCO[[email protected]](C2=CC=CC=C2)(C3=CC=C(Cl)C=C3)C)CCC1.O=C(O)/C=C/C(O)=O

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 : 14.29 mg/mL (31.07 mM; Need ultrasonic)

H2O : 0.67 mg/mL (1.46 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1741 mL 10.8705 mL 21.7410 mL
5 mM 0.4348 mL 2.1741 mL 4.3482 mL
10 mM 0.2174 mL 1.0871 mL 2.1741 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: ≥ 1.43 mg/mL (3.11 mM); Clear solution

  • 2.

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

    Solubility: ≥ 1.43 mg/mL (3.11 mM); Clear solution

  • 3.

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

    Solubility: ≥ 1.43 mg/mL (3.11 mM); Clear solution

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

Purity: 99.95%

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Keywords:

ClemastineHS-592MeclastineHS592HS 592Histamine ReceptorAutophagyInhibitorinhibitorinhibit

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Clemastine fumarate
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HY-B0298A
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