Albamycinsodium

SKU: orb1226203

Description

Novobiocin Sodium is an antibiotic compound derived from Streptomyces niveus.(In Vitro):Bosentan (BOS) competitively and specifically antagonizes binding of 125I-labelled ET-1 to ETA receptors on human smooth muscle cells (SMC) and ETB receptors on human placenta cells. The in vitro binding affinity of Bosentan to ETA receptors on human SMC is 4.7 nM and to ETB receptors on human SMC or placenta cells is 41 or 95 nM. Bosentan has 67-fold greater selectivity for ETA than ETB receptors (mean IC50=7.1 vs 474.8 nM) in an in vitro 125I-labeling assay.(In Vivo):Single-dose Bosentan 62.5 mg significantly (p<0.01 vs baseline) plasma ET-1 levels by 2-fold in 7 pts with WHO class II or III idiopathic or CTD-associated PAH, with peak levels achieved at 8 h. In hypertensive rats, Macitentan 30 mg/kg further decreases mean arterial blood pressure (MAP) by 19 mm Hg when given on top of Bosentan 100 mg/kg. Conversely, Bosentan given on top of Macitentan fails to induce an additional MAP decrease. In pulmonary hypertensive rats, Macitentan 30 mg/kg further decreases mean pulmonary artery pressure (MPAP) by 4 mm Hg on top of Bosentan, whereas a maximal effective dose of Bosentan given on top of Macitentan does not cause any additional MPAP decrease.

Images & Validation

−

Key Properties

−

CAS Number	1476-53-5
MW	634.61
Purity	>98% (HPLC)
Formula	C₃₁H₃₅N₂NaO₁₁
SMILES	[Na+].CO[C@@H]1[C@@H](OC(=O)N)[C@@H](O)[C@H](Oc2ccc3C(=C(NC(=O)c4ccc(O)c(CC=C(C)C)c4)C(=O)Oc3c2C)[O-])OC1(C)C
Target	ABC
Solubility	Ethanol: 127 mg/mL (200.12 mM); Water: 127 mg/mL (200.12 mM); DMSO: 127 mg/mL (200.12 mM)

Bioactivity

−

In Vivo

Novobiocin sodium (25, 50, 100, 200 mg/kg; s. c. ; 4 times at 1, 5, 24 and 48 h after infection) shows anti-infection activity in mice infected with amoxicillin-resistant Streptococcus pneumoniae. Animal model: 30 g adult female Swiss mice (sepsis induced by the penicillin-susceptible strain (AR33118)). Dosage: 25, 50, 100, 200 mg/kg. Administration: S. c. ; given at 1, 5, 24 and 48 h after infection. Result: Showed anti-infection activity in mice infected with amoxicillin-resistant S. pneumoniae.

In Vitro

Novobiocin sodium (1 mM) competitively inhibits ATP binding to gyrase B to interfere with nucleotide binding and interferes with the association of the co-chaperones Hsc70 and p23 with Hsp90.Novobiocin sodium (200 μM; 24 h) inhibits the rate of repair of both cis-DDP and BCNU induced DNA interstrand cross-links and with a corresponding decrease in the clonogenic survival of the human glioblastoma multiforme cells. Novobiocin sodium (0.3 mM; 48 hours) induces a caspase-3/7 enzyme-dependent apoptosis assays with an induction of approximately three- to fivefold of apoptotic cells in K562, HL60, Mutz-2. Western blot analysis. Cell line: K562, HL60, Mutz-2 cells. Concentration: 0.3 mM Incubation time: 48 hours. Result: Decreased caspase-3/7 activity in K562, HL60, Mutz-2 cells.

Storage & Handling

−

Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

−

NSC 2382

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Quick Database Links

Gene Symbol

ABC

Documents Download

Datasheet

Product Information

Download

Request a Document

Protocol Information

Find More Protocols