BTM-1086 is a potent anti-ulcer and gastric secretory inhibiting agent.

Product information

CAS Number: 72293-17-5

Molecular Weight: 367.51

Formula: C21H25N3OS

Chemical Name: (2R,3S)-3-[(4-methylpiperazin-1-yl)methyl]-2-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-4-one

Smiles: CN1CCN(C[C@@H]2[C@@H](SC3=CC=CC=C3NC2=O)C2C=CC=CC=2)CC1

InChiKey: YGOYABDTPZVXLE-XLIONFOSSA-N

InChi: InChI=1S/C21H25N3OS/c1-23-11-13-24(14-12-23)15-17-20(16-7-3-2-4-8-16)26-19-10-6-5-9-18(19)22-21(17)25/h2-10,17,20H,11-15H2,1H3,(H,22,25)/t17-,20+/m1/s1

Technical Data

Appearance: Solid Power

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

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Functional and binding experiments shows that the (-) enantiomer (BTM-1086) has a high affinity (pKi=8.31-9.15) for the three muscarinic receptor subtypes in guinea-pig cortex (M1), heart (M2) and salivary glands (M3).

In Vivo:

BTM-1086 prevents the development of ulcer at a dose of 0.1 to 1 mg/kg, p.o., but only weakly inhibits the histamine induced gastric ulcer. The inhibitory activities of BTM-1086 are significantly higher than those of atropine sulfate. In the healing experiment with the acetic acid-induced stomach ulcer, BTM-1086 (1 mg/kg/day , p.o., x14) shows a significant healing effect, which is higher than that of propantheline bromide . BTM-1086 at a dose of 0.2 mg/kg , i.d., remarkably inhibits the gastric secretion 6 hr after pylorus ligation. The aspirin-induced reductions of the total acid and K+ as well as the increments of the volume and Na+ in the gastric secretion are prevented dose-dependently by pretreatment with BTM-1086. The LD50 value by oral, s.c., and i.v. administration with this compound is 880, 630 and 113 mg/kg, respectively, for male rats and 830, 650 and 119 mg/kg, respectively, for female rats.

Products are for research use only. Not for human use.