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B157

BQ-788

≥95%, endothelin-B (ETRB) blocker, solid

Synonym(s):

2,6-Dimethylpiperidinecarbonyl-γ-Methyl-Leu-Nin-(Methoxycarbonyl)-D-Trp-D-Nle, N-[N-[N-[(2,6-Dimethyl-1-piperidinyl)carbonyl]-4-methyl-L-leucyl]-1-(methoxycarbonyl)-D-tryptophyl]-D-norleucine sodium salt

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About This Item

Empirical Formula (Hill Notation):
C34H50N5NaO7
CAS Number:
Molecular Weight:
663.78
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.32
MDL number:
Assay:
≥95%
Form:
solid
Quality level:
Pricing and availability is not currently available.
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Product Name

BQ-788, ≥95%, solid

Quality Level

assay

≥95%

form

solid

color

white

solubility

acetonitrile: 0.3 mg/mL, DMSO: 1.2 mg/mL, ethanol: 1.2 mg/mL, H2O: slightly soluble

storage temp.

−20°C

SMILES string

[Na+].CCCC[C@@H](NC(=O)[C@@H](Cc1cn(C(=O)OC)c2ccccc12)NC(=O)[C@H](CC(C)(C)C)NC(=O)N3[C@@H](C)CCC[C@H]3C)C([O-])=O

InChI

1S/C34H51N5O7.Na/c1-8-9-16-25(31(42)43)35-29(40)26(18-23-20-38(33(45)46-7)28-17-11-10-15-24(23)28)36-30(41)27(19-34(4,5)6)37-32(44)39-21(2)13-12-14-22(39)3;/h10-11,15,17,20-22,25-27H,8-9,12-14,16,18-19H2,1-7H3,(H,35,40)(H,36,41)(H,37,44)(H,42,43);/q;+1/p-1/t21-,22+,25-,26-,27+;/m1./s1

InChI key

QCVIFBRTTLMEOV-FUKQNADPSA-M

Gene Information

human ... EDNRB(1910)
mouse ... EDNRB(13618)
rat ... EDNRB(50672)

Application

BQ-788 has been used as a selective endothelin-B (ETRB) blocker in human airway smooth muscle cells (HASMCs),[1] uterine mesothelial cells (UtMCs)-derived vascular smooth muscle cells (VSMCs),[2] and human umbilical vein endothelial cells (HUVECs)[3]

Biochem/physiol Actions

Selective ETB endothelin receptor antagonist.

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This Item
B150E5411L9167
form

solid

form

lyophilized powder

form

-

form

solid

assay

≥95%

assay

≥99%

assay

≥95% (HPLC)

assay

≥98% (HPLC)

Quality Level

200

Quality Level

200

Quality Level

200

Quality Level

-

storage temp.

−20°C

storage temp.

−20°C

storage temp.

−20°C

storage temp.

2-8°C

solubility

acetonitrile: 0.3 mg/mL, ethanol: 1.2 mg/mL, H2O: slightly soluble, DMSO: 1.2 mg/mL

solubility

-

solubility

DMSO: 10 mg/mL, ethanol: 10 mg/mL, methanol: 10 mg/mL

solubility

DMSO: ~10 mg/mL, H2O: insoluble

color

white

color

-

color

-

color

light brown


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

Eyeshields, Gloves, type N95 (US)



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Ovidiu Constantin Baltatu et al.
Frontiers in physiology, 3, 103-103 (2012-04-25)
Several clinical studies have investigated the potential benefits of endothelin receptor antagonism in chronic pathologies such as diabetic kidney disease. However, fluid retention and edema have been identified as major side effects of endothelin receptor antagonists. In the present study
Takeshi Nakahara et al.
Scientific reports, 10(1), 9510-9510 (2020-06-13)
Endothelin-1 (ET-1) is well known as the most potent vasoconstrictor, and can evoke histamine-independent pruritus. Recently, its involvement in cutaneous inflammation has begun to draw attention. The upregulation of ET-1 expression in the epidermis of human psoriasis patients has been
Emilie Hitzerd et al.
Hypertension (Dallas, Tex. : 1979), 75(3), 877-884 (2019-12-31)
Increasing evidence suggests a role for the ET (endothelin) system in preeclampsia. Hence, blocking this system with endothelin receptor antagonists (ERAs) could be a therapeutic strategy. Yet, clinical studies are lacking due to possible teratogenic effects of ERAs. In this



Global Trade Item Number

SKUGTIN
B157-200UG04061833426203

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