Pemirolast potassium
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MedKoo CAT#: 319614

CAS#: 100299-08-9 (potassium)

Description: Pemirolast potassium, also known as BMY 26517, is a potent histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent. It has also been studied for the treatment of asthma. Pemirolast potently attenuates paclitaxel hypersensitivity reactions through inhibition of the release of sensory neuropeptides in rats. Pemirolast reduces cisplatin-induced kaolin intake in rats.

Chemical Structure

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Pemirolast potassium
CAS# 100299-08-9 (potassium)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 319614
Name: Pemirolast potassium
CAS#: 100299-08-9 (potassium)
Chemical Formula: C10H7KN6O
Exact Mass: 0.00
Molecular Weight: 266.305
Elemental Analysis: C, 45.10; H, 2.65; K, 14.68; N, 31.56; O, 6.01

Price and Availability

Size Price Availability Quantity
500mg USD 250
1g USD 450
2g USD 750
5g USD 1350
10g USD 2150
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Related CAS #: 69372-19-6 (free base); 100299-08-9 (potassium); 69372-22-1 (Na)  

Synonym: BMY 26517; BMY 26517; BMY 26517; Pemirolast; Pemirolast potassium. trade name: Alegysal and Alamast.

IUPAC/Chemical Name: potassium 5-(9-methyl-4-oxo-4H-pyrido[1,2-a]pyrimidin-3-yl)tetrazol-1-ide

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

SMILES Code: O=C1C(C2=NN=NN2[K])=CN=C3N1C=CC=C3C

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Product Data:
Product Data
Instruction:
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Biological target: Pemirolast potassium (TWT-8152) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.
In vitro activity: An antiallergic drug, pemirolast potassium (TBX) at concentrations between 0.01 and 10 micrograms/ml inhibited antigen (Ag)-stimulated degranulation in RBL-2H3 cells, which have the properties of mucosal mast cells. At the same concentrations, the drug suppressed both the formation of inositol 1,4,5-trisphosphate and the mobilization of Ca2+, indicating the prevention of phospholipase C activation. The production of 1,2-diacylglycerol and phosphatidic acid, which was mainly due to phosphatidylcholine hydrolysis, was also suppressed. Moreover, TBX reduced Ag-induced liberation of arachidonic acid, a precursor of eicosanoids, implying the inhibition of phospholipase A2. These data suggest that TBX inhibits the activation of phospholipase C, leading to decreased formation of the signal transducing molecules necessary for cell activation. Reference: Arerugi. 1994 Feb;43(2 Pt 1):142-51. https://pubmed.ncbi.nlm.nih.gov/8147717/
In vivo activity: The present study investigated the effect of pemirolast on cisplatin-induced kaolin intake, which is an index of nausea/vomiting in the rat. Cisplatin-induced kaolin intake was significantly reduced by co-administration of ondansetron (2 mg/kg, i.p.), a 5-HT(3) receptor antagonist, and dexamethasone (2 mg/kg, i.p.) from days 1 to 5. Similarly, pemirolast (10 mg/kg, p.o.) and the tachykinin NK(1) receptor antagonist aprepitant (10 and 30 mg/kg, p.o.) significantly reduced cisplatin-induced kaolin intake on days 3 and 4. Moreover, pemirolast at the same dose significantly reversed the cisplatin-induced increase in the cerebrospinal fluid level of substance P in rats. Reference: Eur J Pharmacol. 2011 Jul 1;661(1-3):57-62. https://pubmed.ncbi.nlm.nih.gov/21539837/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMF 0.1 0.38
DMSO 1.0 3.76
PBS (pH 7.2) 10.0 37.55
Water 51.5 193.39

Preparing Stock Solutions

The following data is based on the product molecular weight 266.31 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Fujimiya H, Nakashima S, Kumada T, Nakamura Y, Miyata H, Nozawa Y. An antiallergic drug, pemirolast potassium, inhibits inositol 1,4,5-trisphosphate production and Ca2+ mobilization in antigen-stimulated rat basophilic leukemia (RBL-2H3) cells. Arerugi. 1994 Feb;43(2 Pt 1):142-51. PMID: 8147717. 2. Kawashima T, Iwamoto I, Nakagawa N, Tomioka H, Yoshida S. Inhibitory effect of pemirolast, a novel antiallergic drug, on leukotriene C4 and granule protein release from human eosinophils. Int Arch Allergy Immunol. 1994;103(4):405-9. doi: 10.1159/000236662. PMID: 8130655. 3. Tatsushima Y, Egashira N, Matsushita N, Kurobe K, Kawashiri T, Yano T, Oishi R. Pemirolast reduces cisplatin-induced kaolin intake in rats. Eur J Pharmacol. 2011 Jul 1;661(1-3):57-62. doi: 10.1016/j.ejphar.2011.04.026. Epub 2011 Apr 27. PMID: 21539837. 4. Itoh Y, Sendo T, Hirakawa T, Takasaki S, Goromaru T, Nakano H, Oishi R. Pemirolast potently attenuates paclitaxel hypersensitivity reactions through inhibition of the release of sensory neuropeptides in rats. Neuropharmacology. 2004 May;46(6):888-94. doi: 10.1016/j.neuropharm.2003.11.018. PMID: 15033348.
In vitro protocol: 1. Fujimiya H, Nakashima S, Kumada T, Nakamura Y, Miyata H, Nozawa Y. An antiallergic drug, pemirolast potassium, inhibits inositol 1,4,5-trisphosphate production and Ca2+ mobilization in antigen-stimulated rat basophilic leukemia (RBL-2H3) cells. Arerugi. 1994 Feb;43(2 Pt 1):142-51. PMID: 8147717. 2. Kawashima T, Iwamoto I, Nakagawa N, Tomioka H, Yoshida S. Inhibitory effect of pemirolast, a novel antiallergic drug, on leukotriene C4 and granule protein release from human eosinophils. Int Arch Allergy Immunol. 1994;103(4):405-9. doi: 10.1159/000236662. PMID: 8130655.
In vivo protocol: 1. Tatsushima Y, Egashira N, Matsushita N, Kurobe K, Kawashiri T, Yano T, Oishi R. Pemirolast reduces cisplatin-induced kaolin intake in rats. Eur J Pharmacol. 2011 Jul 1;661(1-3):57-62. doi: 10.1016/j.ejphar.2011.04.026. Epub 2011 Apr 27. PMID: 21539837. 2. Itoh Y, Sendo T, Hirakawa T, Takasaki S, Goromaru T, Nakano H, Oishi R. Pemirolast potently attenuates paclitaxel hypersensitivity reactions through inhibition of the release of sensory neuropeptides in rats. Neuropharmacology. 2004 May;46(6):888-94. doi: 10.1016/j.neuropharm.2003.11.018. PMID: 15033348.

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1: Tatsushima Y, Egashira N, Matsushita N, Kurobe K, Kawashiri T, Yano T, Oishi R. Pemirolast reduces cisplatin-induced kaolin intake in rats. Eur J Pharmacol. 2011 Jul 1;661(1-3):57-62. doi: 10.1016/j.ejphar.2011.04.026. Epub 2011 Apr 27. PubMed PMID: 21539837.

2: Gohda T, Ra C, Hamada C, Tsuge T, Kawachi H, Tomino Y. Suppressive activity of pemirolast potassium, an antiallergic drug, on glomerulonephritis. Studies in glomerulonephritis model rats and in patients with chronic glomerulonephritis concurrently affected by allergic rhinitis. Arzneimittelforschung. 2008;58(1):18-23. doi: 10.1055/s-0031-1296461. PubMed PMID: 18368946.

3: Yahata H, Saito M, Sendo T, Itoh Y, Uchida M, Hirakawa T, Nakano H, Oishi R. Prophylactic effect of pemirolast, an antiallergic agent, against hypersensitivity reactions to paclitaxel in patients with ovarian cancer. Int J Cancer. 2006 May 15;118(10):2636-8. PubMed PMID: 16353140.

4: Minami K, Hossen MA, Kamei C. Increasing effect by simultaneous use of levocabastine and pemirolast on experimental allergic conjunctivitis in rats. Biol Pharm Bull. 2005 Mar;28(3):473-6. PubMed PMID: 15744071.

5: Miyake-Kashima M, Takano Y, Tanaka M, Satake Y, Kawakita T, Dogru M, Asano-Kato N, Fukagawa K, Fujishima H. Comparison of 0.1% bromfenac sodium and 0.1% pemirolast potassium for the treatment of allergic conjunctivitis. Jpn J Ophthalmol. 2004 Nov-Dec;48(6):587-90. PubMed PMID: 15592786.

6: Gous P, Ropo A. A comparative trial of the safety and efficacy of 0.1 percent pemirolast potassium ophthalmic solution dosed twice or four times a day in patients with seasonal allergic conjunctivitis. J Ocul Pharmacol Ther. 2004 Apr;20(2):139-50. PubMed PMID: 15117570.

7: Itoh Y, Sendo T, Hirakawa T, Takasaki S, Goromaru T, Nakano H, Oishi R. Pemirolast potently attenuates paclitaxel hypersensitivity reactions through inhibition of the release of sensory neuropeptides in rats. Neuropharmacology. 2004 May;46(6):888-94. PubMed PMID: 15033348.

8: Ohsawa H, Noike H, Kanai M, Hitsumoto T, Aoyagi K, Sakurai T, Sugiyama Y, Yoshinaga K, Kaku M, Matsumoto J, Iizuka T, Shimizu K, Takahashi M, Tomaru T, Sakuragawa H, Tokuhiro K. Preventive effect of an antiallergic drug, pemirolast potassium, on restenosis after stent placement: quantitative coronary angiography and intravascular ultrasound studies. J Cardiol. 2003 Jul;42(1):13-22. PubMed PMID: 12892037.

9: Shulman DG. Two mast cell stabilizers, pemirolast potassium 0.1% and nedocromil sodium 2%, in the treatment of seasonal allergic conjunctivitis: a comparative study. Adv Ther. 2003 Jan-Feb;20(1):31-40. PubMed PMID: 12772816.

10: Abelson MB, Berdy GJ, Mundorf T, Amdahl LD, Graves AL; Pemirolast study group. Pemirolast potassium 0.1% ophthalmic solution is an effective treatment for allergic conjunctivitis: a pooled analysis of two prospective, randomized, double-masked, placebo-controlled, phase III studies. J Ocul Pharmacol Ther. 2002 Oct;18(5):475-88. PubMed PMID: 12419098.

11: Yoshinuma M. [Preventive mechanisms and effects of pemirolast potassium on restenosis after percutaneous transluminal coronary angioplasty: serial coronary angiography and intravascular ultrasound studies]. J Cardiol. 1999 Feb;33(2):81-8. Japanese. PubMed PMID: 10087476.

12: Ohsawa H, Noike H, Kanai M, Yoshinuma M, Mineoka K, Hitsumoto T, Aoyagi K, Sakurai T, Sato S, Uchi T, Kawamura K, Tokuhiro K, Uchida Y, Tomioka H. Preventive effects of an antiallergic drug, pemirolast potassium, on restenosis after percutaneous transluminal coronary angioplasty. Am Heart J. 1998 Dec;136(6):1081-7. PubMed PMID: 9842024.

13: Miyazawa N, Umemura K, Kondo K, Nakashima M. Effects of pemirolast and tranilast on intimal thickening after arterial injury in the rat. J Cardiovasc Pharmacol. 1997 Aug;30(2):157-62. PubMed PMID: 9269941.

14: Nakamura Y, Nakashima S, Fujimiya H, Kumada T, Ojio K, Miyata H, Nozawa Y. [Effects of antiallergic drug, pemirolast potassium on phospholipase D activation in antigen-stimulated rat basophilic leukemia (RBL-2H3) cells]. Arerugi. 1995 Jun;44(6):624-9. Japanese. PubMed PMID: 7669001.

15: Nakamura Y, Nakashima S, Fujimiya H, Kumada T, Kato Y, Miyata H, Nozawa Y. Effects of an antiallergic drug, pemirolast potassium on tyrosine phosphorylation and map kinase activation in antigen-stimulated rat basophilic leukemia (RBL-2H3) cells. Arerugi. 1995 Jan;44(1):34-44. PubMed PMID: 7702453.

16: Nakagawa Y, Jikuhara Y, Higasida M, Yuasa T. [Suppression of conjunctival provocation by 0.1% pemirolast potassium ophthalmic solution in VKC]. Arerugi. 1994 Dec;43(12):1405-8. Japanese. PubMed PMID: 7535044.

17: Fujimiya H, Nakashima S, Kumada T, Nakamura Y, Miyata H, Nozawa Y. An antiallergic drug, pemirolast potassium, inhibits inositol 1,4,5-trisphosphate production and Ca2+ mobilization in antigen-stimulated rat basophilic leukemia (RBL-2H3) cells. Arerugi. 1994 Feb;43(2 Pt 1):142-51. PubMed PMID: 8147717.

18: Kawashima T, Iwamoto I, Nakagawa N, Tomioka H, Yoshida S. Inhibitory effect of pemirolast, a novel antiallergic drug, on leukotriene C4 and granule protein release from human eosinophils. Int Arch Allergy Immunol. 1994;103(4):405-9. PubMed PMID: 8130655.

19: Hasegawa T, Takagi K, Nadai M, Ogura Y, Nabeshima T. Kinetic interaction between theophylline and a newly developed anti-allergic drug, pemirolast potassium. Eur J Clin Pharmacol. 1994;46(1):55-8. PubMed PMID: 8005187.

20: Kemp JP, Bernstein IL, Bierman CW, Li JT, Siegel SC, Spangenberg RD, Tinkelman DG. Pemirolast, a new oral nonbronchodilator drug for chronic asthma. Ann Allergy. 1992 Jun;68(6):488-91. PubMed PMID: 1610024.