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

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

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

Clemastine (HS-592) fumarate is a selective histamine H1 receptor antagonist. Clemastine fumarate is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects.

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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Solution
10 mM * 1 mL in DMSO USD 73 In-stock
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500 mg USD 195 In-stock
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Based on 4 publication(s) in Google Scholar

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Description

Clemastine (HS-592) fumarate is a selective histamine H1 receptor antagonist. Clemastine fumarate is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects[1][2].

IC50 & Target[1]

H1 Receptor

 

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

Appearance

Solid

Formula

C25H30ClNO5
CAS No.
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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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

  • 4.

    Add each solvent one by one:  PBS

    Solubility: 1.43 mg/mL (3.11 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.95%

COA (258 KB) LCMS (128 KB)

Handling Instructions (2659 KB)
References
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Help & FAQs
  • 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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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

Clemastine14976-57-9HS-592MeclastineHS592HS 592Histamine ReceptorantihistamineH1 receptoranti-inflammatoryoralallergic reactionsInhibitorinhibitorinhibit

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