R9028
Repaglinide
≥98% (HPLC), K-ATP channel blocker, solid
동의어(들):
(S)-(+)-2-Ethoxy-4-[N-[1-(2-piperidinophenyl)-3-methyl-1-butyl]aminocarbonylmethyl]benzoic acid, Novonorm, Prandin
조직 및 계약 가격을 보려면 로그인를 클릭합니다.
크기 선택
제품정보 (DICE 배송 시 비용 별도)
실험식(Hill 표기법):
C27H36N2O4
CAS 번호:
Molecular Weight:
452.59
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
제품 이름
Repaglinide, ≥98% (HPLC), solid
SMILES string
CCOc1cc(CC(=O)N[C@@H](CC(C)C)c2ccccc2N3CCCCC3)ccc1C(O)=O
InChI key
FAEKWTJYAYMJKF-QHCPKHFHSA-N
InChI
1S/C27H36N2O4/c1-4-33-25-17-20(12-13-22(25)27(31)32)18-26(30)28-23(16-19(2)3)21-10-6-7-11-24(21)29-14-8-5-9-15-29/h6-7,10-13,17,19,23H,4-5,8-9,14-16,18H2,1-3H3,(H,28,30)(H,31,32)/t23-/m0/s1
assay
≥98% (HPLC)
form
solid
color
white
mp
129-130.2 °C
solubility
DMSO: >20 mg/mL
originator
Novo Nordisk
storage temp.
2-8°C
Quality Level
Gene Information
human ... ABCC8(6833), KCNJ1(3758), KCNJ11(3767)
유사한 제품을 찾으십니까? 방문 제품 비교 안내
관련 카테고리
General description
Repaglinide belongs to the meglitinide class, which differs from the glibenclamide by having a bulky B site group instead of A site.
Application
Repaglinide has been used as a ATP-sensitive potassium channel (KATP) inhibitor in breast cancer cell line MDA-MB-231. It has also been used in the preparation of KATP complex to study its interaction using cryo-EM structural analysis.
Biochem/physiol Actions
Repaglinide (RPG) due to its fast-acting effect prevents hypoglycemia. The KATP inhibition by RPG leads to depolarization in pancreatic β cells leading in voltage-gated calcium channel activation triggering insulin release. Repaglinide favors calcein passage and improves the gap junctional intercellular communication (GJIC). Structurally, RPG binds to the ABC transporter sulfonylurea receptor 1 (SUR1) in the transmembrane bundle.
Repaglinide is a potent short-acting insulin secretagogue that acts by closing ATP-sensitive potassium (KATP) channels in the plasma membrane of the pancreatic beta cell.
Repaglinide is a potent short-acting insulin secretagogue that acts by closing ATP-sensitive potassium (KATP) channels in the plasma membrane of the pancreatic beta cell. It represents a new class of insulin secretagogues, structurally unrelated to sulphonylureas, which were developed for the treatment of type 2 diabetes.
Features and Benefits
This compound is a featured product for ADME Tox research. Click here to discover more featured ADME Tox products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound was developed by Novo Nordisk. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
저장 등급
11 - Combustible Solids
wgk
WGK 2
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
Fatima Maqoud et al.
Pharmaceutics, 13(9) (2021-09-29)
Zoledronic acid (ZOL) is used as a bone-specific antiresorptive drug with antimyeloma effects. Adverse drug reactions (A.D.R.) are associated with ZOL-therapy, whose mechanics are unknown. ZOL is a nitrogen-containing molecule whose structure shows similarities with nucleotides, ligands of ATP-sensitive K+
Thomas M Bodenstine et al.
FEBS letters, 586(1), 27-31 (2011-11-29)
Gap junctional intercellular communication (GJIC) regulates cellular homeostasis by propagating signaling molecules, exchanging cellular metabolites, and coupling electrical signals. In cancer, cells exhibit altered rates of GJIC which may play a role in neoplastic progression. K(ATP) channels help maintain membrane
Mechanism of pharmacochaperoning in a mammalian KATP channel revealed by cryo-EM
Martin GM, et al.
eLife, 8 (2019)
Deaths in trials should always be reported.
Jeppe Schroll
BMJ (Clinical research ed.), 347, f4219-f4219 (2013-07-06)
Carolina Säll et al.
Drug metabolism and disposition: the biological fate of chemicals, 40(7), 1279-1289 (2012-03-28)
Repaglinide is presently recommended by the U.S. Food and Drug Administration as a clinical CYP2C8 probe, yet current in vitro and clinical data are inconsistent concerning the role of this enzyme in repaglinide elimination. The aim of the current study
문서
Discover Bioactive Small Molecules for ADME/Tox
관련 콘텐츠
자사의 과학자팀은 생명 과학, 재료 과학, 화학 합성, 크로마토그래피, 분석 및 기타 많은 영역을 포함한 모든 과학 분야에 경험이 있습니다..
고객지원팀으로 연락바랍니다.