WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H412139
CAS#: 39577-20-3 (HCl)
Description: Picumast dihydrochloride is a prophylactically active anti-allergic compound which combines inhibition of mediator release and action. The activity profile of PDH differs clearly from that of known prophylactic anti-allergic drugs such as DSCG and ketotifen.
Hodoodo Cat#: H412139
Name: Picumast dihydrochloride
CAS#: 39577-20-3 (HCl)
Chemical Formula: C25H31Cl3N2O3
Exact Mass: 0.00
Molecular Weight: 513.884
Elemental Analysis: Chemical Formula: Exact Mass: Molecular Weight: Elemental Analysis: C, 58.43; H, 6.08; Cl, 20.70; N, 5.45; O, 9.34
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Related CAS #: 39577-20-3 (HCl) 39577-19-0 (free base)
Synonym: Picumast dihydrochloride; BM-15100; BM15100; BM 15100 ; BM-15,100; BM15,100; BM 15,100
IUPAC/Chemical Name: 2H-1-Benzopyran-2-one, 7-(3-(4-((4-chlorophenyl)methyl)-1-piperazinyl)propoxy)-3,4-dimethyl-, dihydrochloride
InChi Key: AMHVERUFVROLJA-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H29ClN2O3.2ClH/c1-18-19(2)25(29)31-24-16-22(8-9-23(18)24)30-15-3-10-27-11-13-28(14-12-27)17-20-4-6-21(26)7-5-20;;/h4-9,16H,3,10-15,17H2,1-2H3;2*1H
SMILES Code: O=C1C(C)=C(C)C2=CC=C(OCCCN3CCN(CC4=CC=C(Cl)C=C4)CC3)C=C2O1.[H]Cl.[H]Cl
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
Shelf Life: >3 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:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 513.88 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.
| 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: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Wilhelms OH, Roesch A, Schaumann W. Picumast dihydrochloride (Auteral), a new anti-allergic inhibitor of mediator release and action. Agents Actions Suppl. 1991;34:335-49. PMID: 1686528.
2: Hockwin O, Müller-Breitenkamp U, Laser H, Messinger D, Goder G, Meinel U. Lens safety study with Picumast dihydrochloride--a double masked study using the Scheimpflug method. Lens Eye Toxic Res. 1990;7(3-4):625-30. PMID: 1983108.
3: Boerner D, Metz K, Eberhardt R. Acceptability, safety and efficacy of picumast dihydrochloride on long-term use in patients with perennial bronchial asthma. Arzneimittelforschung. 1989 Oct;39(10A):1372-4. PMID: 2576367.
4: Slapke J, Müller S, Boerner D. A one-year double-blind clinical study of the efficacy and tolerability of picumast dihydrochloride versus ketotifen in patients with bronchial asthma. Arzneimittelforschung. 1989 Oct;39(10A):1368-72. PMID: 2576366.
5: Boerner D, Metz K, Eberhardt R. Efficacy and tolerability of picumast dihydrochloride in comparison with placebo in asthmatic patients. Arzneimittelforschung. 1989 Oct;39(10A):1363-7. PMID: 2576365.
6: Franke W, Messinger D. Double-blind multicenter controlled clinical study comparing the efficacy of picumast dihydrochloride versus astemizole and placebo in patients with seasonal allergic rhinitis. Arzneimittelforschung. 1989 Oct;39(10A):1360-3. PMID: 2576364.
7: Boerner D, Metz K, Eberhardt R, Schürmann W. A placebo-controlled comparison of the efficacy and tolerability of picumast dihydrochloride and terfenadine in patients with seasonal allergic rhinitis. Arzneimittelforschung. 1989 Oct;39(10A):1356-9. PMID: 2576363.
8: Franke W, Bachert C, Messinger D. Double-blind controlled crossover study comparing the protective effect of picumast dihydrochloride versus placebo following nasal allergen challenge. Arzneimittelforschung. 1989 Oct;39(10A):1354-6. PMID: 2576362.
9: Herberg KW. Double-blind study on the influence of picumast dihydrochloride on safety-related performance. Arzneimittelforschung. 1989 Oct;39(10A):1348-51. PMID: 2576361.
10: Neugebauer G, Raedsch R, Stiehl A, Kaufmann B, Besenfelder E, Neubert P, Walter-Sack I. Pharmacokinetics of picumast dihydrochloride in patients with liver cirrhosis. Arzneimittelforschung. 1989 Oct;39(10A):1343-7. PMID: 2576360.
11: Wittenbrink-Dix AM, Neugebauer G, Fuhr U, Neubert P, Besenfelder E, Woelke- Seidl E, Harder S, Staib AH. Study of potential kinetic interactions of picumast dihydrochloride and theophylline in vitro and after oral administration in man. Arzneimittelforschung. 1989 Oct;39(10A):1339-43. PMID: 2576359.
12: Neugebauer G, Wittenbrink-Dix AM, Woelke-Seidl E, Kaufmann B, Ponton T, Dahmen W, Mosberg H, Nieder N, Besenfelder E. Pharmacokinetics of picumast dihydrochloride and its active metabolites M1 and M2 in humans. Arzneimittelforschung. 1989 Oct;39(10A):1336-9. PMID: 2576358.
13: Abraham WM. Effect of picumast dihydrochloride on antigen-induced early and late airway responses in allergic sheep. Arzneimittelforschung. 1989 Oct;39(10A):1328-31. PMID: 2576357.
14: Schaumann W, Besenfelder E, Boehm E, Neubert P, Roesch A, Sterz H. Pharmacokinetics of picumast after administration of 14C-picumast dihydrochloride in dogs, rats, rabbits and monkeys. Arzneimittelforschung. 1989 Oct;39(10A):1321-7. PMID: 2576356.
15: Besenfelder E, Neubert P, Roesch A, Schaumann W, Wilhelms OH. Metabolism of picumast after administration of picumast dihydrochloride and antiallergic activity of the main metabolites. Arzneimittelforschung. 1989 Oct;39(10A):1317-20. PMID: 2576355.
16: Roesch A, Schaumann W, Wilhelms OH. Antiallergic activity of picumast dihydrochloride in several animal species. Arzneimittelforschung. 1989 Oct;39(10A):1310-6. PMID: 2576354.
17: Witte EC. Chemical synthesis of picumast dihydrochloride. Arzneimittelforschung. 1989 Oct;39(10A):1309. PMID: 2576353.
18: Zimmermann I, Roesch A, Ulmer WT. Influence of picumast dihydrochloride on the ex vivo histamine release from leucocytes of allergic asthmatic patients. Arzneimittelforschung. 1989 Oct;39(10A):1351-3. PMID: 2483313.
19: Sekardi L, Friedberg KD. Inhibition of immunological histamine release from guinea pig lungs and other organs by mepyramine, ketotifen, and picumast in vivo. Arzneimittelforschung. 1989 Oct;39(10A):1331-5. PMID: 2483312.
