SGLT
There are six SGLT proteins identified in human, Despite the prominent sequence homology between SGLT1 and SGLT2, they exhibit distinct physiological and biochemical properties. SGLT1 is primarily expressed in intestine, while SGLT2 is highly expressed in the kidney cortex and plays an important role in reabsorption of glucose in kidney. The major substrates of SGLT1 are both glucose and galactose, whereas SGLT2 prefers glucose to galactose. SGLT1 mutations are found in patients with glucose–galactose malabsorption. Mutations of SGLT2 are associated with the genetic disease Familial Renal Glucosuria. The characterizations of other SGLTs are rather preliminary. Interestingly, SGLT3 has no glucose transport activity, but may serve as a glucose sensor in the enteric nervous system. SGLT4 exhibits higher affinity for mannose than glucose and may function as a mannose transporter. SGLT5, which is highly expressed in kidney cortex, also has a substrate preference for mannose. SGLT6, also known as SMIT2 (myoinositol:Na1 symporter), transports inositol instead of glucose.
References
1.Deng D, et al. Protein Sci. 2016;25(3):546–558.
References
1.Deng D, et al. Protein Sci. 2016;25(3):546–558.
GPCR/G Protein
ACAT(3)
Angiotensin Receptor(27)
Antibacterial(545)
Bombesin Receptor(13)
Bradykinin Receptor(23)
Calcium Channel(197)
cAMP(16)
Cannabinoid Receptor(88)
CaSR(18)
CGRP Receptor(18)
Chemokine Receptor(104)
Cholecystokinin Receptor(24)
CRF Receptor(15)
Dopamine Receptor(182)
Endothelin Receptor(28)
FFAR(5)
Galanin Receptor(1)
GHSR(20)
Glucagon Receptor(51)
GPCR19(9)
GPR119(3)
Hedgehog (Hh)(35)
Histamine Receptor(139)
Imidazoline Receptor(1)
Leukotriene Receptor(15)
LHR(1)
LPA Receptor(19)
Lysophospholipid Receptor(13)
mAChR(25)
MCHR(8)
Melanocortin Receptor(28)
Melatonin Receptor(7)
Motilin Receptor(4)
Neurokinin Receptor(43)
Neuropeptide Y Receptor(44)
Neurotensin Receptor(11)
Orexin Receptor(16)
Other Targets(3)
OXTR(2)
P2Y Receptor(14)
PAR(28)
Platelet-activating Factor Receptor(2)
Prostaglandin Receptor(79)
PTH Receptor(1)
S1P Receptor(35)
SGLT(26)
Somatostatin Receptor(16)
Urotensin Receptor(4)
Vasopressin Receptor(20)
SGLT
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Sergliflozin A
产品货号 : M36251
cas no: 360775-96-8
Sergliflozin A is a selective SGLT2 inhibitor that induces diabetes in a dose-dependent manner. It reduces hyperglycemia. -
O-Desethyl Dapagliflozin
产品货号 : M36025
cas no: 864070-37-1
O-Desethyl Dapagliflozin (Empagliflozin-4) is a SGLT2 inhibitor, IC50=33nM. -
Remogliflozin etabonate
产品货号 : M34693
cas no: 442201-24-3
Remogliflozin etabonate (GSK189075) 是一种具有口服活性的,选择性和低亲和力的钠葡萄糖共转运蛋白 (SGLT2) 抑制剂,对 hSGLT2,rSGLT2,hSGLT1,rSGLT1 的 Ki 值分别为 1.95 μM,43.1 μM,2.14 μM,8.57 μM。Remogliflozin etabonate 是一种基于苄基吡唑葡糖苷的前体,在体内被代谢成其活性形式,瑞格列净 (Remogliflozin)。Remogliflozin etabonate 在啮齿动物模型中显示出抗糖尿病功效。 -
Canagliflozin hemihydrate
产品货号 : M33547
cas no: 928672-86-0
Canagliflozin hemihydrate (JNJ28431754 hemihydrate) 是一种选择性的 SGLT2 抑制剂,作用于表达 mSGLT2,rSGLT2 和 hSGLT2 的 CHO细胞,IC50 分别为 2 nM,3.7 nM 和 4.4 nM。 -
Leachianone A
产品货号 : M29179
cas no: 97938-31-3
Leachianone A 是一种潜在的抗毒剂,它对镉诱导的细胞毒性具有抑制作用。