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Cat. No. | Product Name | Target | Signaling Pathways |
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T11418 |
Glucokinase activator 1
|
Others | Others |
Glucokinase activator 1 is a liver-directed glucokinase activator (EC50: 34 nM). | |||
T72284 |
Glucokinase activator 3
|
||
Glucokinase activator3 是Glucokinase (GK) 的一种高效全效激活剂,AC50 值为 38 nM,具有研究 2 型糖尿病潜力。 | |||
TQ0055 |
AMG-3969
|
Glucokinase | Metabolism |
AMG-3969 是一种葡萄糖激酶-葡糖激酶调节蛋白相互作用的干扰物,IC50=为4 nM。 | |||
T3312 |
AM-2394
AM2394 |
Glucokinase | Metabolism |
AM-2394 是新型的 glucokinase 激活剂 (GKA)。它能够激活葡萄糖激酶 (GK),EC50=60 nM。 | |||
T16479 |
PF-04937319
|
Others; Glucokinase | Metabolism; Others |
PF-04937319 是一种葡萄糖激酶激活剂 (EC50 =154.4 μM)。 PF-04937319 保持降糖功效,同时降低许多其他 GKA 观察到的低血糖风险。 PF-04937319可用于治疗2型糖尿病的研究。 | |||
T3104 |
Globalagliatin
LY2608204 |
Glucokinase | Metabolism |
Globalagliatin (LY2608204) 是一种葡萄糖激酶 (GK) 活化剂,EC50=42 nM。 | |||
T15159 |
Dorzagliatin
HMS5552 |
Glucokinase | Metabolism |
Dorzagliatin (HMS5552) 是双重作用的葡萄糖激酶 (glucokinase;GK) 激活剂,可改善 2 型糖尿病的血糖控制,提高胰腺 β 细胞功能。 | |||
T26712 |
AZD-1656
AZD 1656 |
Glucokinase | Metabolism |
AZD-1656 是口服有效的葡萄糖激酶选择性激活剂,EC50为 60 nM。AZD1656在2 型糖尿病中有研究的价值。 | |||
T12056 |
MK-0941 free base
|
Glucokinase | Metabolism |
MK-0941 free base 是一种口服具有活力的葡糖激酶抑制剂,在葡萄糖浓度为 2.5 和 10 mM 的条件下,对重组人 glucokinase 的EC50值分别为 240 和 65 nM。它具有较强的降血糖特性,是研究 2 型糖尿病的候选药物。 | |||
T68762 |
LY-2599506
|
||
LY-2599506 is a novel glucokinase activator. | |||
T30142 |
ARRY-403
AMG-151,ARRY 403,ARRY403,ARRY-403,AMG151,AMG 151 |
Glucokinase | Metabolism |
ARRY-403 是一种新型葡萄糖激酶激活剂,可降低 2 型糖尿病患者的空腹和餐后血糖,可用于治疗糖尿病。 | |||
T77784 |
WAY-297848
|
Glucokinase | Metabolism |
WAY-297848 是一种新型的 glucokinase 激活剂,可用于预防或治疗高血糖、糖尿病、肥胖症、血脂异常和代谢综合征。 | |||
T3104L |
(1S,2R)-Globalagliatin
(1S,2R)-Globalagliatin(1S,2R-1234703-40-2) |
Glucokinase | Metabolism |
(1S,2R)-Globalagliatin 是一种高效的葡萄糖激酶 (GK) 激活剂,可用于研究 2 型糖尿病。 | |||
T14212 |
AMG-1694
|
Glucokinase | Metabolism |
AMG-1694 是一种强效的葡萄糖激酶-葡萄糖激酶调节蛋白(GK-GKRP)干扰物,能促进 GK-GKRP 复合物的解离,其 IC50 值为 7 nM,从而间接提高 GK 酶的活性。AMG-1694 可使几种啮齿动物糖尿病模型的血糖水平恢复正常,并降低糖尿病动物而非正常血糖动物的血糖。AMG-1694 能有效逆转 GKRP 对 GK 活性的抑制作用,并促进 GK 转位。 | |||
T29974 | AMG-7549 | ||
AMG-7549 is a disrupter of Glucokinase−Glucokinase Regulatory Protein (GK−GKRP) binding. | |||
T68244 |
PF-04279405
|
||
PF-04279405 is a potent and selective glucokinase activator. | |||
T10092 | PSN-GK1 | Others | Others |
PSN-GK1 is a potent activator of glucokinase (EC50: 0.13 μM). | |||
T28781 |
Sinogliatin
HMS-5552,RO 5305552,HMS5552,RO5305552,HMS 5552,RO-5305552 |
||
Sinogliatin, a glucokinase activator, is used potentially for the treatment of type 2 diabetes. | |||
T23765 |
AZD1092
AZD 1092,AZD-1092 |
||
AZD1092 is the glucokinase enzyme activator. | |||
T16480 |
PF-04991532
|
Glucokinase | Metabolism |
PF-04991532 is an effective, hepatoselective glucokinase activator. It has EC50s of 80 and 100 nM in human and rat, respectively. | |||
T25451 |
GKA-22
GKA22,GKA 22 |
||
GKA-22 is a human glucokinase allosteric activator in the absence of glucose. | |||
T25452 |
GKA-71
GKA 71 |
||
GKA-71 is an effective glucokinase activator (GKA). | |||
T32612 |
LBX192
NVP-LBX-192,LBX-192,LBX 192,NVP-LBX192,NVP-LBX 192 |
||
LBX192( NVP-LBX192) is a liver-targeted glucokinase activator. | |||
T11401 |
GKA50
|
Others | Others |
GKA50 stimulates insulin release from mouse islets of Langerhans and MIN6 cells. GKA50 shows significant glucose lowering in high fat fed female rats. GKA50 is a potent glucokinase activator (EC50=33 nM at 5 mM glucose). | |||
T64046 | BMS-820132 | ||
BMS-820132 是一种葡萄糖激酶 (glucokinase) 激活剂 (AC50: 29 nM)。 | |||
T10362 |
AR453588
|
Others | Others |
AR453588 is an orally bioavailable anti-diabetic glucokinase activator (EC50: 42 nM) with anti-hyperglycemic activity. | |||
T10362L |
AR453588 hydrochloride
|
Others | Others |
AR453588 hydrochloride is an orally bioavailable anti-diabetic glucokinase activator (EC50: 42 nM) with anti-hyperglycemic activity. | |||
T26718 |
AZD6370
AZD-6370,AZD 6370 |
||
AZD-6370 is a glucokinase activator. AZD-6370 decreases fasting and postprandial glucose in type 2 diabetes mellitus patients with effects influenced by dosing regimen and food. AZD-6370 do not affect the central counterregulatory response to hypoglycemia | |||
T12057 |
MK-0941
|
Others | Others |
MK-0941 is an orally active and allosteric glucokinase activator, has potential in the treatment of type 2 diabetes. | |||
T70639 |
AM-9514
|
||
AM-9514 is a novel, potent Glucokinase (GK) activator. AM-9514 showed a favorable combination of in vitro potency, enzyme kinetic properties, acceptable pharmacokinetic profiles in preclinical species, and robust efficacy in a rodent PD model. Glucokinase (GK) activators represent a class of type 2 diabetes therapeutics actively pursued due to the central role that GK plays in regulating glucose homeostasis. | |||
T70391 |
AMG151 HCl
|
||
ARRY-403, also known as AMG-151, is an orally available allosteric glucokinase (GK) activator developed for the treatment of type 2 diabetes mellitus (T2DM). ARRY-403 has many favorable physicochemical characteristics and ADME properties (low potential to cause drug–drug interactions (DDIs). ARRY-403 potently activates human glucokinase (GK) in vitro (EC50 = 79 nM at 5 mM glucose), with an S0.5 = 0.93 mM glucose (ARRY-403 at 5 mM) and Vmax = 134% compared to the no activator control. It possesse... | |||
T72743 |
(R)-PF-04991532
|
||
(R)-PF-04991532 是PF-04991532 的 R 型异构体。PF-04991532 是一种有效的肝选择性葡萄糖激酶激活剂。 | |||
T68976 | Piragliatin | ||
Piragliatin, also known as RO4389620, is a glucokinase activator. Piragliatin greatly enhances glucose-induced pancreatic islet respiration and insulin release. Piragliatin lowers plasma glucose both in the postabsorptive state and after a glucose challenge in patients with type 2 diabetes mellitus. Piragliatin has an acute glucose-lowering action in patients with mild type 2 diabetes, mainly mediated through a generalized enhancement of β-cell function and through fasting restricted changes in ... | |||
T63019 | GKA50 quarterhydrate | ||
GKA50 quarterhydrate 是一种有效的葡萄糖激酶激活剂,其 EC50 值为 33 nM。GKA50 quarterhydrate 是一种啮齿动物和人类胰岛中 β 细胞代谢的葡萄糖样激活剂,也是一种 Ca2+依赖性胰岛素分泌调节剂。GKA50 quarterhydrate 能够刺激小鼠胰岛分泌胰岛素,可以显著降低高脂喂养的雌性大鼠血糖。 |
Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T19500 |
Palmitelaidic Acid
trans-Palmitoleic acid,9-trans-Hexadecenoic acid,软脂酸 |
Glucokinase; AMPK; PPAR | Chromatin/Epigenetic; DNA Damage/DNA Repair; Metabolism; PI3K/Akt/mTOR signaling |
trans-Palmitelaidic Acid (trans-Palmitoleic acid) 是palmitoleic acid 的反式异构体。Palmitoleic acid 是血清和组织中最丰富的脂肪酸之一。 | |||
T4726 |
D-Glucose 6-phosphate sodium
G6P sodium salt,D-Glucose 6-phosphate sodium salt,D-葡萄糖-6-磷酸钠盐,Sodium Glucose-6-Phosphate |
Others; Endogenous Metabolite | Metabolism; Others |
D-Glucose 6-phosphate sodium (G6P sodium salt) 是内源性代谢产物的一种。 | |||
T5069 |
D-Glucose 6-phosphate potassium salt
|
Others | Others |
在细胞中,当葡萄糖被己糖激酶或葡萄糖激酶磷酸化或在糖原分解过程中通过磷酸葡萄糖变位酶转化葡萄糖 1-磷酸时,会产生D-glucose 6-phosphate (G6P)。 G6P 位于糖酵解和戊糖磷酸途径的起点。当血糖水平高时,它也可以作为糖原储存。 |