Pemirolast potassium (TWT-8152; BMY 26517)

Alias: TWT-8152; BMY 26517; TWT 8152; BMY 26517; TWT8152; BMY 26517; Pemirolast; Pemirolast potassium. trade name: Alegysal and Alamast.
Cat No.:V1241 Purity: ≥98%
Pemirolast potassium (formerly TWT 8152; BMY 26517; TWT-8152; BMY-26517; Alegysal and Alamast), the potassium salt of Pemirolast, is a poten and orally bioactive histamine H1 antagonist and mast cell stabilizer with potential antiallergic effects.
Pemirolast potassium (TWT-8152; BMY 26517) Chemical Structure CAS No.: 100299-08-9
Product category: Histamine Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
50mg
100mg
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Other Forms of Pemirolast potassium (TWT-8152; BMY 26517):

  • Pemirolast
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Pemirolast potassium (formerly TWT 8152; BMY 26517; TWT-8152; BMY-26517; Alegysal and Alamast), the potassium salt of Pemirolast, is a poten and orally bioactive histamine H1 antagonist and mast cell stabilizer with potential antiallergic effects. For the treatment of asthma, a nonbronchodilator antiallergy medication candidate is being researched.

Biological Activity I Assay Protocols (From Reference)
Targets
Histamine H1 receptor
ln Vitro

In vitro activity: Pemirolast potassium (BMY 26517) is a brand-new oral nonbronchodilator antiallergy drug that's currently being tested for use in treating asthma. In addition to being shown to inhibit the release of peptides such as substance P, [2] neurokinin (NK) A, and calcitonin gene-related peptide (CGRP) from sensory nerves, pemirolast potassium (BMY 26517) also inhibits the release of chemical mediators from tissue mast cells.[3] In order to prevent pulmonary hypersensitivity reactions to medications like paclitaxel, pemirolast potassium is used as a treatment for allergic conjunctivitis.[4]

ln Vivo
Pemirolast potassium (BMY 26517) inhibits the release of substance P in rats, thereby reducing their intake of kaolin. [2] Pemirolast inhibits the release of sensory neuropeptides in rats, thereby potently attenuating hypersensitivity reactions to paclitaxel. [3]
Animal Protocol

Rats
References

[1]. Ann Allergy . 1992 Jun;68(6):488-91.

[2]. Eur J Pharmacol . 2011 Jul 1;661(1-3):57-62.

[3]. Neuropharmacology . 2004 May;46(6):888-94.

[4]. J Ocul Pharmacol Ther . 2002 Oct;18(5):475-88.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C10H7KN6O
Molecular Weight
266.3
Exact Mass
266.03
Elemental Analysis
C, 45.10; H, 2.65; K, 14.68; N, 31.56; O, 6.01
CAS #
100299-08-9
Related CAS #
Pemirolast; 69372-19-6
Appearance
Solid powder
SMILES
CC1=CC=CN2C1=NC=C(C2=O)C3=NN=N[N-]3.[K+]
InChi Key
NMMVKSMGBDRONO-UHFFFAOYSA-N
InChi Code
InChI=1S/C10H7N6O.K/c1-6-3-2-4-16-9(6)11-5-7(10(16)17)8-12-14-15-13-8;/h2-5H,1H3;/q-1;+1
Chemical Name
potassium;9-methyl-3-(1,2,3-triaza-4-azanidacyclopenta-2,5-dien-5-yl)pyrido[1,2-a]pyrimidin-4-one
Synonyms
TWT-8152; BMY 26517; TWT 8152; BMY 26517; TWT8152; BMY 26517; Pemirolast; Pemirolast potassium. trade name: Alegysal and Alamast.
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: <1 mg/mL
Water: ~53 mg/mL (~199.0 mM)
Ethanol: <1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: 100 mg/mL (375.52 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.7552 mL 18.7758 mL 37.5516 mL
5 mM 0.7510 mL 3.7552 mL 7.5103 mL
10 mM 0.3755 mL 1.8776 mL 3.7552 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02517372 Completed Drug: CRD007 Healthy Volunteers RSPR Pharma AB October 2014 Phase 1
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