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34

抑制剂 & 化合物

3

天然产物

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Cat. No. Product Name Target Signaling Pathways
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 GlucokinaseGlucokinase 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。

化合物

Glucokinase activator 1
Cat.No: T11418
Synonym:
Target: Others
Glucokinase activator 3
Cat.No: T72284
Synonym:
Target:
AMG-3969
Cat.No: TQ0055
Synonym:
Target: Glucokinase
AM-2394
Cat.No: T3312
Synonym: AM2394
Target: Glucokinase
PF-04937319
Cat.No: T16479
Synonym:
Target: Others, Glucokinase
Globalagliatin
Cat.No: T3104
Synonym: LY2608204
Target: Glucokinase
Dorzagliatin
Cat.No: T15159
Synonym: HMS5552
Target: Glucokinase
AZD-1656
Cat.No: T26712
Synonym: AZD 1656
Target: Glucokinase
MK-0941 free base
Cat.No: T12056
Synonym:
Target: Glucokinase
LY-2599506
Cat.No: T68762
Synonym:
Target:
ARRY-403
Cat.No: T30142
Synonym: AMG-151,ARRY 403,ARRY403,ARRY-403,AMG151,AMG 151
Target: Glucokinase
WAY-297848
Cat.No: T77784
Synonym:
Target: Glucokinase
(1S,2R)-Globalagliatin
Cat.No: T3104L
Synonym: (1S,2R)-Globalagliatin(1S,2R-1234703-40-2)
Target: Glucokinase
AMG-1694
Cat.No: T14212
Synonym:
Target: Glucokinase
AMG-7549
Cat.No: T29974
Synonym:
Target:
PF-04279405
Cat.No: T68244
Synonym:
Target:
PSN-GK1
Cat.No: T10092
Synonym:
Target: Others
Sinogliatin
Cat.No: T28781
Synonym: HMS-5552,RO 5305552,HMS5552,RO5305552,HMS 5552,RO-5305552
Target:
AZD1092
Cat.No: T23765
Synonym: AZD 1092,AZD-1092
Target:
PF-04991532
Cat.No: T16480
Synonym:
Target: Glucokinase
GKA-22
Cat.No: T25451
Synonym: GKA22,GKA 22
Target:
GKA-71
Cat.No: T25452
Synonym: GKA 71
Target:
LBX192
Cat.No: T32612
Synonym: NVP-LBX-192,LBX-192,LBX 192,NVP-LBX192,NVP-LBX 192
Target:
GKA50
Cat.No: T11401
Synonym:
Target: Others
BMS-820132
Cat.No: T64046
Synonym:
Target:
AR453588
Cat.No: T10362
Synonym:
Target: Others
AR453588 hydrochloride
Cat.No: T10362L
Synonym:
Target: Others
AZD6370
Cat.No: T26718
Synonym: AZD-6370,AZD 6370
Target:
MK-0941
Cat.No: T12057
Synonym:
Target: Others
AM-9514
Cat.No: T70639
Synonym:
Target:
AMG151 HCl
Cat.No: T70391
Synonym:
Target:
(R)-PF-04991532
Cat.No: T72743
Synonym:
Target:
Piragliatin
Cat.No: T68976
Synonym:
Target:
GKA50 quarterhydrate
Cat.No: T63019
Synonym:
Target:
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。

天然产物

Palmitelaidic Acid
Cat.No: T19500
Synonym: trans-Palmitoleic acid,9-trans-Hexadecenoic acid,软脂酸
Target: Glucokinase, AMPK, PPAR
D-Glucose 6-phosphate sodium
Cat.No: T4726
Synonym: G6P sodium salt,D-Glucose 6-phosphate sodium salt,D-葡萄糖-6-磷酸钠盐,Sodium Glucose-6-Phosphate
Target: Others, Endogenous Metabolite
D-Glucose 6-phosphate potassium salt
Cat.No: T5069
Synonym:
Target: Others
TargetMol Loading
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