1. Immunology/Inflammation
    GPCR/G Protein
    Autophagy
  2. Histamine Receptor
    Autophagy

Clemastine fumarate (Synonyms: Meclastine fumarate)

Cat. No.: HY-B0298A Purity: 99.82%
Handling Instructions

Clemastine 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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
100 mg USD 60 In-stock
200 mg USD 96 In-stock
500 mg USD 197 In-stock
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5 g   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Clemastine Fumarate is a selective histamine H1 receptor antagonist with IC50 of 3 nM. Target: Histamine H1 Receptor Clemastine 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].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume 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.
References
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

Storage
Pure form -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Clemastine fumarate
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HY-B0298A
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