Batimastat sodium salt |
| カタログ番号GC35470 |
Batimastat ナトリウム塩は、MMP-1、MMP-2、MMP-9、MMP-7、および MMP-3 に対してそれぞれ 3、4、4、6、および 20 nM の IC50 を持つ強力な広域スペクトル MMP 阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 130464-84-5
Sample solution is provided at 25 µL, 10mM.
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Batimastat sodium salt is a potent broad spectrum MMP inhibitor with IC50 of 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, respectively. IC50: 3 nM (MMP-1), 4 nM (MMP-2), 4 nM (MMP-9), 6 nM (MMP-7), 20 nM (MMP-3)[1]
Batimastat (BB-94) is a potent matrix metalloproteinase inhibitor, exhibits an unexpected mode of binding. Batimastat inhibits gelatinases A and B with IC50 values of 4 nM and 10 nM, respectively. The IC50 with the structurally similar collagenase Ht-d is 6 nM, which is comparable with values for MMP-1 (3 nM), MMP-8 (10 nM), and MMP-3 (20 nM)[2]. CD30 shedding from the cell line Karpas299 can effectively be blocked by the hydroxamic acidbased metalloproteinase inhibitor Batimastat (BB-94, IC50=230 nM)[3].
Intraperitoneal administration of Batimastat (BB-94) effectively blocks growth of human ovarian carcinoma xenografts and murine melanoma metastasis and delays the growth of primary tumors in an orthotopic model of human breast cancer without cytotoxicity and without affecting mRNA levels[2]. Batimastat (BB-94) is a synthetic matrix metalloproteinase inhibitor that has shown antineoplastic and antiangiogenic activity in various tumor models. Treatment with Batimastat (60 mg/kg i.p. every other day, for a total of eight injections) concomitantly with Cisplatin (4 mg/kg i.v., every 7 days for a total of three injections) completely prevents growth and spread of both xenografts, and all animals are alive and healthy on day 200[4]. Kaplan-Meier analysis of survival (at 48 h) shows that animals treated with Batimastat (BB-94) have increased survival (95.2%) in comparison with controls (75%), and differences are almost statistically significant (p=0.064)[5]. Matrix density is analyzed in saline- or Batimastat (40 mg/kg)-pretreated animals 4 h after E2 administration, the time point at which collagen density is observed to be at its lowest after hormone treatment[6].
[1]. Yin Z, et al. Increased MMPs expression and decreased contraction in the rat myometrium during pregnancy and in response to prolonged stretch and sex hormones. Am J Physiol Endocrinol Metab. 2012 Jul 1;303(1):E55-70. [2]. Botos I, et al. Batimastat, a potent matrix mealloproteinase inhibitor, exhibits an unexpected mode of binding. Proc Natl Acad Sci U S A. 1996 Apr 2;93(7):2749-54. [3]. Hansen HP, et al. Inhibition of metalloproteinases enhances the internalization of anti-CD30 antibody Ki-3 and the cytotoxic activity of Ki-3 immunotoxin. Int J Cancer. 2002 Mar 10;98(2):210-5. [4]. Giavazzi R, et al. Batimastat, a synthetic inhibitor of matrix metalloproteinases, potentiates the antitumor activity of cisplatin in ovarian carcinoma xenografts. Clin Cancer Res. 1998 Apr;4(4):985-92. [5]. Ricci S, et al. Inhibition of matrix metalloproteinases attenuates brain damage in experimental meningococcal meningitis. BMC Infect Dis. 2014 Dec 31;14:726. [6]. Russo LA, et al. Regulated expression of matrix metalloproteinases, inflammatory mediators, and endometrial matrix remodeling by 17beta-estradiol in the immature rat uterus. Reprod Biol Endocrinol. 2009 Nov 4;7:124.
Animal experiment: | Mice[5] Six-weeks-old female BALB/c mice are used. Mice are treated i.p. with Batimastat (BB-94, 50 mg/kg) 1 h before and 24 h post-infection. Batimastat is suspended at 50 mg/mL in DMSO and stored frozen at -20°C. Prior to use, it is diluted 20-fold in phosphate buffered saline (PBS), and 500 μL are injected into animals. Control mice are injected with 500 μL of 5% DMSO in PBS. Animals are sacrificed 48 h after i.c. challenge. Rats[6] Female Sprague-Dawley rats are administered a single physiological dose of E2 (40 μg/kg in a 0.9% NaCl, 0.4% EtOH vehicle) by intraperitoneal (i.p.) injection at the indicated time intervals prior to tissue collection at necropsy. This in vivo dose level of E2 has been shown to induce changes in uterine wet weight, tissue architecture, and gene expression characteristic of estrogen receptor activation. For all other experiments, animals are i.p. administered a single 40 μg/kg bolus of E2 4 h prior to tissue harvest, while control animals receive vehicle only in all studies. Batimastat is administered i.p. at a dose level (40 mg/kg in a 1× PBS, 0.1% Tween-20 vehicle) shown to be effective at inhibiting MMPs in vivo 4 h prior to E2 or saline control. |
References: [1]. Yin Z, et al. Increased MMPs expression and decreased contraction in the rat myometrium during pregnancy and in response to prolonged stretch and sex hormones. Am J Physiol Endocrinol Metab. 2012 Jul 1;303(1):E55-70. | |
| Cas No. | 130464-84-5 | SDF | |
| Canonical SMILES | [O-]NC([C@@H](CSC1=CC=CS1)[C@@H](CC(C)C)C(N[C@@H](CC2=CC=CC=C2)C(NC)=O)=O)=O.[Na+] | ||
| Formula | C23H30N3NaO4S2 | M.Wt | 499.62 |
| 溶解度 | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0015 mL | 10.0076 mL | 20.0152 mL |
| 5 mM | 0.4003 mL | 2.0015 mL | 4.003 mL |
| 10 mM | 0.2002 mL | 1.0008 mL | 2.0015 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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 ddH2O, 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 24 reference(s) in Google Scholar.)
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