Bestatin , 10mMinDMSO , 58970-76-6
Synonym(s):
([2S,3R]-3-Amino-2-hydroxy-4-phenylbutanoyl)-L -leucine;[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutanoyl]-Leu;N-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutyryl]-L -leucine hydrochloride;Bestatin hydrochloride;N-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutyryl]-L -leucine hydrochloride
CAS NO.：58970-76-6
Empirical Formula: C16H24N2O4
Molecular Weight: 308.37
MDL number: MFCD00083262
EINECS: 261-529-2
| Pack Size | Price | Stock | Quantity |
| 1ml | RMB159.20 | In Stock |
|
| others | Enquire |
PRODUCT Properties
| Melting point: | 245 °C (dec.)(lit.) |
| alpha | D20 -15.5° (c = 1.0 in 1N HCl) |
| Boiling point: | 448.76°C (rough estimate) |
| Density | 1.0917 (rough estimate) |
| refractive index | 1.5800 (estimate) |
| storage temp. | Keep in dark place,Sealed in dry,Room Temperature |
| solubility | Aqueous Acid (Slightly, Sonicated), DMSO (Slightly, Heated) |
| pka | 8.1, 3.1(at 25℃) |
| form | Powder |
| color | White |
| optical activity | [α]20/D 11°, c = 1 in 1 M NaOH |
| Water Solubility | Soluble in water (<1 25), DMSO (2 mg/ml), methanol (5 mg/ml), 1eq. NaOH (50 mM), ethanol (<1 mg/ml at 25°C), acetic acid, aq. HCl, and alkaline solution. Insoluble in ethyl acetate, benzene, hexane, and chloroform. |
| Merck | 13,9910 |
| InChIKey | VGGGPCQERPFHOB-RDBSUJKOSA-N |
| CAS DataBase Reference | 58970-76-6(CAS DataBase Reference) |
Description and Uses
Bestatin is an aminopeptidase inhibitor originally isolated from S. olivoreticuli. It inhibits aminopeptidase B (IC50 = 0.05 μg/ml), aminopeptidase N (IC50 = 16.9 μM), leucine aminopeptidase (IC50 = 0.01 μg/ml), and the aminopeptidase activity of leukotriene A4 (LTA4) hydrolase (Kapp = 172 nM). It is selective for these aminopeptidases over aminopeptidase A, trypsin, chymotrypsin, elastase, papain, pepsin, and thermolysin. Bestatin inhibits the production of LTB4 in erythrocytes when used at a concentration of 70 μM. It increases the expression of Akt, inhibits proliferation, migration, and invasion, and induces autophagy and apoptosis in 5637 bladder cancer cells. Bestatin (5 and 15 mg/kg) decreases serum levels of LTB4 and reduces tumor growth in a patient-derived xenograft (PDX) mouse model of colorectal cancer.
Bestatin is "pseudo"-dipeptide isolated from Strepotmyces olivreticuli in 1976. Bestatin is a potent aminopeptidase B inhibitor with no carboxypeptidase activity. Bestatin acts as an immunomodulator by activating macrophages and T lymphocytes. Bestatin also exhibits good antitumour activity and is has been investigated in clinical trials.
Safety
| Symbol(GHS) |  GHS07 |
| Signal word | Warning |
| Hazard statements | H315-H319-H335 |
| Precautionary statements | P264b-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P362+P364-P403+P233-P501c |
| Safety Statements | 22-24/25 |
| WGK Germany | 3 |
| RTECS | OH2915000 |
| HS Code | 29242998 |
| Toxicity | LD50 in male, female mice, male, female rats (g/kg): 1.3, 1.9, 1.9, 2.1 s.c.; 0.19, 0.19, 0.90, 0.78 i.p.; >4.0, >4.0, >2.0, >2.0 orally (Sakakibara) |
