Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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B275090-1mg | 1mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $99.90 | |
B275090-5mg | 5mg | In stock | $395.90 | |
B275090-10mg | 10mg | In stock | $692.90 | |
B275090-25mg | 25mg | In stock | $1,559.90 | |
B275090-50mg | 50mg | In stock | $2,806.90 | |
B275090-100mg | 100mg | In stock | $5,051.90 |
Potent, selective ET A receptor antagonist
Synonyms | 2-((3R,6S,9R,12R,17aS)-9-((1H-indol-3-yl)methyl)-6-isobutyl-3-isopropyl-1,4,7,10,13-pentaoxohexadecahydro-1H-pyrrolo[1,2-a][1,4,7,10,13]pentaazacyclopentadecin-12-yl)acetic acid | cyclo(L-Leu-D-Trp-D-Asp-L-Pro-D-Val) | BDBM50197954 | LS-13503 | B-186 | BQ |
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Specifications & Purity | Moligand™, ≥98% |
Biochemical and Physiological Mechanisms | Potent, selective ET A receptor antagonist (IC 50 values are 7.3 and 18,000 nM for ET A and ET B endothelin receptors respectively). Some ability to cross the blood-brain barrier. Anti-ischemic activity in vivo . |
Storage Temp | Store at -20°C,Desiccated |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | ANTAGONIST |
Mechanism of action | Antagonist of ET A receptor |
Note | Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one week. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details. |
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IUPAC Name | 2-[(3R,6R,9S,12R,15S)-6-(1H-indol-3-ylmethyl)-9-(2-methylpropyl)-2,5,8,11,14-pentaoxo-12-propan-2-yl-1,4,7,10,13-pentazabicyclo[13.3.0]octadecan-3-yl]acetic acid |
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INCHI | InChI=1S/C31H42N6O7/c1-16(2)12-21-27(40)33-22(13-18-15-32-20-9-6-5-8-19(18)20)28(41)35-23(14-25(38)39)31(44)37-11-7-10-24(37)29(42)36-26(17(3)4)30(43)34-21/h5-6,8-9,15-17,21-24,26,32H,7,10-14H2,1-4H3,(H,33,40)(H,34,43)(H,35,41)(H,36,42)(H,38,39)/t21-,22+,23+,24-,26+/m0/s1 |
InChi Key | VYCMAAOURFJIHD-PJNXIOHISA-N |
Canonical SMILES | CC(C)CC1C(=O)NC(C(=O)NC(C(=O)N2CCCC2C(=O)NC(C(=O)N1)C(C)C)CC(=O)O)CC3=CNC4=CC=CC=C43 |
Isomeric SMILES | CC(C)C[C@H]1C(=O)N[C@@H](C(=O)N[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C(=O)N1)C(C)C)CC(=O)O)CC3=CNC4=CC=CC=C43 |
PubChem CID | 443289 |
Molecular Weight | 610.7 |
PubChem CID | 443289 |
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Wikipedia | BQ-123 |
CAS Registry No. | 136553-81-6 |
ChEMBL Ligand | CHEMBL314691 |
GPCRdb Ligand | BQ123 |
Enter Lot Number to search for COA:
Find and download the COA for your product by matching the lot number on the packaging.
Lot Number | Certificate Type | Date | Item |
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K2218158 | Certificate of Analysis | Aug 25, 2022 | B275090 |
K2218163 | Certificate of Analysis | Aug 25, 2022 | B275090 |
K2218171 | Certificate of Analysis | Aug 25, 2022 | B275090 |
K2218172 | Certificate of Analysis | Aug 25, 2022 | B275090 |
K2218174 | Certificate of Analysis | Aug 25, 2022 | B275090 |
K2218188 | Certificate of Analysis | Aug 25, 2022 | B275090 |
Solubility | Soluble in water to 1.25 mg/ml |
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Starting at $241.90
1. Maayah ZH et al.. (2020) Breast cancer diagnosis is associated with relative left ventricular hypertrophy and elevated endothelin-1 signaling.. BMC Cancer, 20 (751). [PMID:32787791] |
2. Wu Q et al.. (2018) CT perfusion imaging of cerebral microcirculatory changes following subarachnoid hemorrhage in rabbits: Specific role of endothelin-1 receptor antagonist.. Brain Res, 1701 (196-203). [PMID:30244111] |
3. Kobayashi Y et al.. (2021) Early manifestations and differential gene expression associated with photoreceptor degeneration in Prom1-deficient retina.. Dis Model Mech, 14 (11): [PMID:34664634] |
4. Furukawa A et al.. (2018) Endothelin Signaling Contributes to Modulation of Nociception in Early-stage Tongue Cancer in Rats.. Anesthesiology, 128 (6): (1207-1219). [PMID:29461271] |