1. Materials information
Use of Chlorpheniramine maleate
Chlorpheniramine maleate is an histamine H1 receptor antagonist with IC50 of 12 nM.Target: Histamine H1 ReceptorChlorpheniramine inhibits the proliferation of MCF-7, MDA-MB 231, and Ehrlich cells in a dose-response manner, and significantly reduces the ornithine decarboxylase mRNA translation by 50%-70% at the 250 μM [1]. Chlorpheniramine displaces of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells with IC50 of 66 nM. Chlorpheniramine displays antimalarial activity against CQS strain (D6) and MDR strain (Dd2) of P. falciparum with IC50 of 61.2 uM and 3.9 uM, respectively. Chlorpheniramine displays cytotoxicity against the proliferation of concanavalin A-induced murine splenic lymphocytes with IC50 of 33.4 μM [2].Oral administration of Chlorpheniramine inhibits histamine-induced mortality in guinea pigs with an ED50 of 0.17 mg/kg [3]. Oral administration of Chlorpheniramine (10 mg/kg) significantly inhibits short-duration scratching in BALB/c mice stimulated by ovalbumin active cutaneous anaphylaxis and in ICR mice subcutaneously injected with histamine, but not long-duration scratching seen in NC/Nga mice, in contrast to that of dexamethasone or tacrolimus [4].
Chlorpheniramine maleate Biological Activity
| Description | Chlorpheniramine maleate is an histamine H1 receptor antagonist with IC50 of 12 nM.Target: Histamine H1 ReceptorChlorpheniramine inhibits the proliferation of MCF-7, MDA-MB 231, and Ehrlich cells in a dose-response manner, and significantly reduces the ornithine decarboxylase mRNA translation by 50%-70% at the 250 μM [1]. Chlorpheniramine displaces of [3H]pyrilamine from human histamine receptor subtype 1 expressed in CHO cells with IC50 of 66 nM. Chlorpheniramine displays antimalarial activity against CQS strain (D6) and MDR strain (Dd2) of P. falciparum with IC50 of 61.2 uM and 3.9 uM, respectively. Chlorpheniramine displays cytotoxicity against the proliferation of concanavalin A-induced murine splenic lymphocytes with IC50 of 33.4 μM [2].Oral administration of Chlorpheniramine inhibits histamine-induced mortality in guinea pigs with an ED50 of 0.17 mg/kg [3]. Oral administration of Chlorpheniramine (10 mg/kg) significantly inhibits short-duration scratching in BALB/c mice stimulated by ovalbumin active cutaneous anaphylaxis and in ICR mice subcutaneously injected with histamine, but not long-duration scratching seen in NC/Nga mice, in contrast to that of dexamethasone or tacrolimus [4]. |
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| Related Catalog | Signaling Pathways >> GPCR/G Protein >> Histamine Receptor Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor Research Areas >> Inflammation/Immunology |
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| References | [1]. Medina, M.A., et al., Chlorpheniramine inhibits the synthesis of ornithine decarboxylase and the proliferation of human breast cancer cell lines. Breast Cancer Res Treat, 1995. 35(2): p. 187-94. [2]. Kelly, J.X., et al., Design, synthesis, and evaluation of 10-N-substituted acridones as novel chemosensitizers in Plasmodium falciparum. Antimicrob Agents Chemother, 2007. 51(11): p. 4133-40. [3]. Iemura, R., et al., Synthesis of 2-(4-substituted-1-piperazinyl)benzimidazoles as H1-antihistaminic agents. J Med Chem, 1986. 29(7): p. 1178-83. [4]. Takano, N., I. Arai, and M. Kurachi, Analysis of the spontaneous scratching behavior by NC/Nga mice: a possible approach to evaluate antipruritics for subjects with atopic dermatitis. Eur J Pharmacol, 2003. 471(3): p. 223-8. |
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Chemical & Physical Properties
| Density | 1.1±0.1 g/cm3 |
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| Boiling Point | 379.0±42.0 °C at 760 mmHg |
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| Melting Point | 130-135 °C(lit.) |
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| Molecular Formula | C20H23ClN2O4 |
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| Molecular Weight | 390.861 |
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| Flash Point | 183.0±27.9 °C |
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| Exact Mass | 390.134644 |
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| PSA | 90.73000 |
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| LogP | 3.39 |
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| Vapour Pressure | 0.0±0.9 mmHg at 25°C |
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| Index of Refraction | 1.565 |
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| Storage condition | -20°C Freezer |
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| Water Solubility | 1-5 G/100 ML AT 21 ºC |
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2. Packaging of materials
For powders: normal is 25kgs/Drum or bag, or larger/smaller package as request.
For liquids: normal 25kgs/drum, 180-300kgs/bucket, or IBC, determined by the nature of the product.
Or smaller package 1kg/bottle, 10kgs/bottle as request.
3. Shipping & Delivery
Provide door to door service
Suitable for goods under 50kg
Delivery: 3-7 days
Cost: low cost
Provide airport to airport service
Suitable for goods over 50kg
Delivery: 3-14 days
Cost: high cost
Provide seaport to seaport service
Suitable for goods over 100kg
Delivery: 2-45 days
Cost: low cost
4. Contact information
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