N-CIS-2,6-DIMETHYLPIPERIDINOCARBONYL-BETA-TBU-ALA-D-TRP(1-METHOXYCARBONYL)-D-NLE-OH
- CAS No.
- 173326-37-9
- Chemical Name:
- N-CIS-2,6-DIMETHYLPIPERIDINOCARBONYL-BETA-TBU-ALA-D-TRP(1-METHOXYCARBONYL)-D-NLE-OH
- Synonyms
- BQ788,BQ 788;BQ788, CID 3081333;N-cis-2,6-DiMethylpiperidinocarbonyl-b-tBu-Ala-D-Trp(1-Methoxycarbonyl)-D-Nle-OH;D-Norleucine, N-[(cis-2,6-dimethyl-1-piperidinyl)carbonyl]-4-methyl-L-leucyl-1-(methoxycarbonyl)-D-tryptophyl- (9CI);D-Norleucine,N-[N-[N-[(2,6-dimethyl-1-piperidinyl)carbonyl]-4-methyl-L-leucyl]-1-(methoxycarbonyl)-D-tryptophyl]-,cis-;(2R)-2-[[(2R)-2-[[(2S)-2-[[(2R,6S)-2,6-dimethylpiperidine-1-carbonyl]amino]-4,4-dimethylpentanoyl]amino]-3-(1-methoxycarbonylindol-3-yl)propanoyl]amino]hexanoicacid;(2R)-2-[[(2R)-2-AMINO-3-(1-METHOXYCARBONYLINDOL-3-YL)PROPANOYL]-[(2S)-2-[[(2R,6S)-2,6-DIMETHYLPIPERIDINE-1-CARBONYL]AMINO]-4,4-DIMETHYLPENTANOYL]AMINO]HEXANOIC ACID
- CBNumber:
- CB41474659
- Molecular Formula:
- C34H51N5O7
- Molecular Weight:
- 641.8
- MDL Number:
- MFCD06245594
- MOL File:
- 173326-37-9.mol
Density | 1.23±0.1 g/cm3(Predicted) |
---|---|
storage temp. | Store at -20°C |
solubility | DMSO: 10 mM |
form | A solid |
pka | 3.40±0.10(Predicted) |
FDA UNII | 6MB0YNA8DJ |
N-CIS-2,6-DIMETHYLPIPERIDINOCARBONYL-BETA-TBU-ALA-D-TRP(1-METHOXYCARBONYL)-D-NLE-OH price More Price(9)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Biosynth Carbosynth | FB108685 | BQ-788 | 173326-37-9 | 500ug | $400 | 2021-12-16 | Buy |
Biosynth Carbosynth | FB108685 | BQ-788 | 173326-37-9 | 1mg | $600 | 2021-12-16 | Buy |
Biosynth Carbosynth | FB108685 | BQ-788 | 173326-37-9 | 2mg | $1100 | 2021-12-16 | Buy |
AK Scientific | 9131CN | BQ-788freeacid | 173326-37-9 | 2mg | $1535 | 2021-12-16 | Buy |
Biosynth Carbosynth | FB108685 | BQ-788 | 173326-37-9 | 5mg | $2600 | 2021-12-16 | Buy |
N-CIS-2,6-DIMETHYLPIPERIDINOCARBONYL-BETA-TBU-ALA-D-TRP(1-METHOXYCARBONYL)-D-NLE-OH Chemical Properties,Uses,Production
Biological Activity
BQ-788 is a potent and selective ETB receptor antagonist with IC50 of 1.2 nM for inhibiting ET-1 binding to the ETB receptor in human Girrardi heart cells.
in vitro
BQ-788 potently and competitively inhibits 125 I-labeled ET-1 binding to ETB receptors in human Girardi heart cells (hGH) with an IC 50 of 1.2 nM, but only poorly inhibits the binding to ETA receptors in human neuro-blastoma cell line SK-N-MC cells (IC 50 , 1300 nM). BQ-788 shows no agonistic activity up to 10 μM and competitively inhibits thevasoconstriction induced by an ETB-selective agonist (pA2, 8.4). BQ-788 also inhibits several bioactivities of ET-1, such as bronchoconstriction, cell proliferation, and clearance of perfused ET-1.
in vivo
BQ-788 (3 mg/kg/h, iv) completely inhibits a pharmacological dose of ET-1- or sarafotoxin6c (0.5 nmol/kg, iv)-induced ETB receptor-mediated depressor, but not pressor responses in conscious rats. Furthermore, BQ-788 markedly increased the plasma concentration of ET-1, which is considered an index of potential ETB receptor blockade in vivo. In Dahl salt-sensitive hypertensive (DS) rats, BQ-788 (3 mg /kg/h, iv) increases blood pressure by about 20 mm Hg. It is reported that BQ-788 also inhibits ET-1-induced bronchoconstriction, tumor growth and lipopolysaccharide-induced organfailure. BQ 788 (3 mg/kg) results in an eightfold leftward shift in the ET-1 dose-response curve, suggesting a significant involvement of ETB dilator receptors. Mice are treated with 30 nmol BQ-788 by intraplantar, reduce mechanical hyperalgesia (47% and 42%), thermal hyperalgesia (68 % and 76%), oedema (50% and 30%); myeloperoxidase activity (64% and 32%), and overt-pain like behaviours. Additionally, intra plantar treatment with clazosentan or BQ-788 decreases spinal (45% and 41%) and peripheral (47% and 47%) superoxide anion production as well as spinal (47% and 47%) and peripheral (33% and 54%) lipid decreases peroxidation, respectively.
target
IC50: 1.2 nM (ETB)
N-CIS-2,6-DIMETHYLPIPERIDINOCARBONYL-BETA-TBU-ALA-D-TRP(1-METHOXYCARBONYL)-D-NLE-OH Preparation Products And Raw materials
Raw materials
Preparation Products
N-CIS-2,6-DIMETHYLPIPERIDINOCARBONYL-BETA-TBU-ALA-D-TRP(1-METHOXYCARBONYL)-D-NLE-OH Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
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TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
Chengdu Youngshe Chemical Co., Ltd. | +8618108235634 | Cecilia@youngshechem.com | China | 2345 | 58 |
LEAP CHEM CO., LTD. | +86-852-30606658 | market18@leapchem.com | China | 24738 | 58 |
Nanjing TGpeptide | +86-13347807150 +86-13347807150 | support@tgpeptide.com | China | 3279 | 58 |
Zhejiang Hangyu API Co., Ltd | +8617531972939 | anna@api-made.com | China | 2944 | 58 |
Hangzhou Sinoda Pharmaceutical Technology Co. LTD | 17306812703 | 3007955328@qq.com | China | 5720 | 58 |
Shanghai Hanhong Scientific Co.,Ltd. | 021-54306202 13764082696; | info@hanhongsci.com | China | 42982 | 64 |
Chemsky (shanghai) International Co.,Ltd | 021-50135380 | shchemsky@sina.com | China | 15421 | 60 |
MedChemexpress LLC | 021-58955995 | sales@medchemexpress.cn | United States | 4863 | 58 |