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[CAS NO. 222638-67-7] BEChydrochloride
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-19548A |
| Brand: | MCE |
| CAS: | 222638-67-7 |
Overview
| MDL | MFCD03453539 |
|---|---|
| Molecular Weight | 229.49 |
| Molecular Formula | C5H13BClNO4S |
| SMILES | N[C@@H](CSCCB(O)O)C(O)=O.[H]Cl |
Summary
IC50 & Target
Ki: 0.31 μM (BEC hydrochloride, at pH 7.5) and 30 nM (BEC hydrochloride, at pH 9.5) [1]
In Vitro
The X-ray crystal structure of the arginase-BEC complex has been determined at 2.3 Å resolution from crystals perfectly twinned by hemihedry. The structure of the complex reveals that the boronic acid moiety undergoes nucleophilic attack by metal-bridging hydroxide ion to yield a tetrahedral boronate anion that bridges the binuclear manganese cluster, thereby mimicking the tetrahedral intermediate (and its flanking transition states) in the arginine hydrolysis reaction [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Administration of the arginase inhibitor BEC decreases arginase activity and causes alterations in NO homeostasis, which are reflected by increases in S-nitrosylated and nitrated proteins in the lungs from inflamed mice. BEC enhances perivascular and peribronchiolar lung inflammation, mucus metaplasia, NF-κB DNA binding, and mRNA expression of the NF-κB-driven chemokine genes CCL20 and KC, and leads to further increases in airways hyperresponsiveness [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | C57BL/6J wild-type mice, mice deficient in arginase 2 (Arg2 -/- ), mice deficient in both arginase 1 and 2 (Arg1 -/- Arg2 -/- ), and mice deficient in NOX2 (NOX2 -/- |
| Dosage: | 20 mg/kg. |
| Administration: | I.V., in 0.9% saline, 1 hour before the injection of LPS. |
| Result: | BEC robustly reduced VEGF expression in neuroglia (72% reduction) and macrophage/microglia (87% reduction). |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 50 mg/mL ( 217.87 mM ; Need ultrasonic)
H 2 O : 5 mg/mL ( 21.79 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.3575 mL | 21.7874 mL | 43.5749 mL |
| 5 mM | 0.8715 mL | 4.3575 mL | 8.7150 mL |
| 10 mM | 0.4357 mL | 2.1787 mL | 4.3575 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 140 mg/mL (610.05 mM); Clear solution; Need ultrasonic
-
2.
-
3.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (10.89 mM); Clear solution
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (10.89 mM); Clear solution
References
- [1] Colleluori DM, et al. Classical and slow-binding inhibitors of human type II arginase. Biochemistry. 2001 Aug 7;40(31):9356-62.
- [2] Kim NN, et al. Probing erectile function: S-(2-boronoethyl)-L-cysteine binds to arginase as a transition state analogue and enhances smooth muscle relaxation in human penile corpus cavernosum. Biochemistry. 2001 Mar 6;40(9):2678-88.
- [3] Ckless K, et al. Inhibition of arginase activity enhances inflammation in mice with allergic airway disease, in association with increases in protein S-nitrosylation and tyrosine nitration. J Immunol. 2008 Sep 15;181(6):4255-64.
Synonyms
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