PZ0318
PF-06761281
≥97% (HPLC)
동의어(들):
(2R)-2-Hydroxy-2-[2-(2-methoxy-5-methyl-3-pyridinyl)ethyl]-butanedioic acid, (R)-2-Hydroxy-2-(2-(2-methoxy-5-methylpyridin-3-yl)ethyl)-succinic acid
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C13H17NO6
CAS Number:
Molecular Weight:
283.28
MDL number:
UNSPSC 코드:
12161503
PubChem Substance ID:
NACRES:
NA.77
추천 제품
Quality Level
분석
≥97% (HPLC)
형태
powder
색상
white to beige
solubility
H2O: 20 mg/mL, clear
배송 상태
dry ice
저장 온도
−20°C
SMILES string
CC1=CC(CC[C@](CC(O)=O)(O)C(O)=O)=C(OC)N=C1
InChI
1S/C13H17NO6/c1-8-5-9(11(20-2)14-7-8)3-4-13(19,12(17)18)6-10(15)16/h5,7,19H,3-4,6H2,1-2H3,(H,15,16)(H,17,18)/t13-/m1/s1
InChI key
FGYMJXFSHBLHLW-CYBMUJFWSA-N
일반 설명
PF-06761281 is a small, polar dicarboxylate compound. Its structure is similar to citrate, which is the endogenous substrate of Na+-citrate cotransporter (NaCT). It is a novel, potent inhibitor of SLC13a2/3/5 (solute channel) family, along with selectivity for NaCT.
애플리케이션
PF-06761281 has been used as a SLC13A family inhibitor, in rats to determine its unbound partition coefficient (Kpuu), to estimate its potency as a drug.
생화학적/생리학적 작용
PF-06761281 is an inhibitor of the sodium-coupled citrate transporter (NaCT or SLC13A5), which may be a target for tretment and prevention of metabolic disorders. The SLC13 transporters SLC13A2 (NaDC1), SLC13A3 (NaDC3), and SLC13A5 (NaCT) co-transport di- and tricarboxylates with multiple sodium ions into cells. PF-06761281 inhibits citrate uptake with an IC50 of 740 nM for NaCT in human hepatocytes. PF-06761281 has >25-fold in vitro selectivity for NaCT over NaDC1 and NaDC3 and was inactive in a selectivity panel of 65 targets.
신호어
Danger
유해 및 위험 성명서
Hazard Classifications
Acute Tox. 3 Oral
Storage Class Code
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
Kim Huard et al.
Journal of medicinal chemistry, 59(3), 1165-1175 (2016-01-07)
Inhibition of the sodium-coupled citrate transporter (NaCT or SLC13A5) has been proposed as a new therapeutic approach for prevention and treatment of metabolic diseases. In a previous report, we discovered dicarboxylate 1a (PF-06649298) which inhibits the transport of citrate in
Determination of Unbound Partition Coefficient and in Vitro-in Vivo Extrapolation for SLC13A Transporter-Mediated Uptake.
Riccardi K et al
Drug Metabolism and Disposition, 44(10), 1633-1642 (2016)
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