BTM-1086 |
Catalog No.GC32039
One-Click Copy Product Info
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BTM-1086 is a potent anti-ulcer and gastric secretory inhibiting agent.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 72293-17-5
Sample solution is provided at 25 µL, 10mM.
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BTM-1086 is a potent anti-ulcer and gastric secretory inhibiting agent.
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)[1].
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[2].
[1]. Eltze M, et al. Affinity profiles of BTM-1086 and BTM-1041 at muscarinic receptor subtypes and at H1- and alpha 1-receptors. Eur J Pharmacol. 1989 Nov 7;170(3):225-34. [2]. Hajimu Y, et al. Antiulcer Effect of (-)-cis-2, 3-Dihydro-3-(4-Methylpiperazinylmethyl)-2-Phenyl-1, 5-Benzothiazepin-4-(5H)-One Hydrochloride (BTM-1086) in Experimental Animals. Japan J Pharmacol. 41, 283-292 (1986).
Animal experiment: | Rats[2]Rats weighing 180 to 190 g are anesthesized with ether and subjected to laparotomy to expose the stomach after which 20 gal of 20% acetic acid is injected carefully under the serous membrane of the abdominal side in the glandular stomach; then the abdomen is closed. Thereafter, the animals are fed normally and 5 mL/kg of BTM-1086 dissolved or suspended in 0.5% gum arabic solution is administered p.o. once daily for 14 days from the second day after the operation. The longitudinal and abscissal length of the areas are quickly measured with a calliper, and the multiplied product is used as the ulcer index[2]. |
References: [1]. Eltze M, et al. Affinity profiles of BTM-1086 and BTM-1041 at muscarinic receptor subtypes and at H1- and alpha 1-receptors. Eur J Pharmacol. 1989 Nov 7;170(3):225-34. | |
| Cas No. | 72293-17-5 | SDF | |
| Canonical SMILES | O=C1[C@H](CN2CCN(C)CC2)[C@H](C3=CC=CC=C3)SC4=CC=CC=C4N1 | ||
| Formula | C21H25N3OS | M.Wt | 367.51 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.721 mL | 13.6051 mL | 27.2101 mL |
| 5 mM | 544.2 μL | 2.721 mL | 5.442 mL |
| 10 mM | 272.1 μL | 1.3605 mL | 2.721 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)