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抑制剂 & 化合物

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Cat. No. Product Name Target Signaling Pathways
T15812 LY2979165

mGlu2 agonist

GluR Neuroscience
LY2979165 (mGlu2 agonist) 是 mGluR2 的正构激动剂,可用于作为抗抑郁药的研究。
T6022 LY404039

pomaglumetad

Glucocorticoid Receptor; GluR Endocrinology/Hormones; Neuroscience
LY404039 (pomaglumetad) 是可口服的mGluR2mGluR3选择性激动剂,有抗精神病和抗焦虑的作用。它对重组人mGluR2mGluR3的Ki 分别为 149 和 92 nM,比对其他受体/转运蛋白的抑制性高 100 倍以上。
T3451 JNJ-42153605

GluR Neuroscience
JNJ42153605是一种代谢型谷氨酸2 (mGlu2) 受体的正变构调节剂,EC50值为17 nM。
T23010 MNI 137

Others; GluR Neuroscience; Others
MNI 137 是 mGlu2 的负变构调节剂。 MNI 137 抑制谷氨酸诱导的钙动员,对人和大鼠的 IC50 分别为 8.3 和 12.6 nM。
T22638 CBiPES hydrochloride

CBiPES HCl

GluR Neuroscience
CBiPES hydrochloride(CBiPES HCl) 是一种高效的 mGlu2 受体正变构调节剂,EC50值为 92.8 nM。CBiPES hydrochloride 可阻断 WT 和 mGlu(3) 受体的作用。CBiPES hydrochloride 可用于研究像癫痫和帕金森综合征类的神经系统疾病。
T20941 Cloransulam-methyl

Cloransulam methyl

Others Others
Cloransulam-methyl 是一种有效的除草剂,常施用于大豆田来防治阔叶杂草。Cloransulam-methyl会在大豆植物中很快代谢掉,却会在土壤中存在。
T23000 ML289

VU0463597,ML 289

GluR Neuroscience
ML289 (VU0463597)是一种高效、选择性的,可透过血脑屏障的 mGlu3 (IC50=0.66 μM) 负变构调节剂。ML289 的选择性是 mGlu2 的 15 倍,对 mGlu5 无活性。
T61972 Pomaglumetad methionil hydrochloride

LY2140023 hydrochloride

GluR Neuroscience
Pomaglumetad methionil hydrochloride (LY2140023 hydrochloride) (LY2140023 hydrochloride) 是的 LY404039 的蛋氨酸前药,具有口服活性。LY404039是一种选择性 mGlu2/3 受体激动剂。Pomaglumetad methionil hydrochloride 可用于精神分裂症的研究。
T6726 VU0361737

ML-128,VU 0361737

GluR Neuroscience
VU0361737 (ML-128) 是一种高效选择性的,中枢神经系统渗透性的代谢型谷氨酸受体 4(mGluR4)正变构调节剂,对人类和大鼠 mGluR4作用的EC50值分别为 240 和 110 nM。它具有神经保护作用,有用于帕金森氏病的研究潜力。
TQ0094 JNJ-40411813

ADX-71149

GluR Neuroscience
JNJ-40411813 (ADX-71149) 是一种新型 mGlu2R 正变构调节剂,EC50 值为 147 nM。
T28928 TASP0433864

TASP0433864 is a positive allosteric modulator of metabotropic glutamate 2 receptor with EC50 values of 199 and 206 nM at human and rat mGlu2 receptors, respectively, without exerting agonist activity at rat mGlu2 receptor.
T23247 Ro 64-5229

Others Others
mGlu2 antagonist
T27686 JNJ-46356479

JNJ 46356479

JNJ-46356479 is a Selective and Orally Bioavailable mGlu2 receptor Positive Allosteric Modulator (PAM). JNJ-46356479 showed mGlu2 PAM EC50=78 nM; mGlu2 PAM Emax (%) = 256.
T15809 LY2812223

LIM Kinase Cell Cycle/Checkpoint
LY2812223 is a highly effective and functionally selective mGlu2 receptor agonist. It has a mGlu2 binding affinity for mGlu2 and mGlu3 (Ki=144 nM and 156 nM, respectively).
T15817 Eglumegad

Eglumetad,LY354740

Others Others
Eglumegad is a highly effective and selective agonist of group II (mGlu2/3) receptor (IC50s: 5 and 24 nM on transfected human mGlu2 and mGlu3 receptors, respectively).
T22955 LY487379 hydrochloride

LY 487379 hydrochloride

Others Others
Positive allosteric modulator of mGlu2 receptors
T29142 VU6001966

VU 6001966,VU-6001966

VU6001966 is a potent and selective mGlu2 inhibitor (mGlu2 IC50 = 78 nM) and negative allosteric modulator. VU6001966 exhibits excellent central nervous system (CNS) penetration.
T29141 VU6001192

VU 6001192,VU-6001192

VU6001192 is a negative allosteric modulator of mGlu2.
T34376 RO5488608

RO 5488608,RO-5488608

RO5488608 is a new type of high-efficiency mGlu2/3 NAM.
T27950 LY389795

LY-389795,LY 389795

LY389795 is an agonist of group II (mGlu2/3) metabotropic glutamate receptor, it is used in inflammatory pain models.
T27680 JNJ-40068782

JNJ 40068782

JNJ-40068782 is a potent, selective and systemically active positive allosteric modulator of the mGlu2 receptor.
T11911 LY3020371 hydrochloride

GluR Neuroscience
LY3020371 hydrochloride exerts an antidepressant-like signature in vivo. LY3020371 hydrochloride is a potent, selective metabotropic glutamate 2/3 receptor (mGlu2/3) antagonist with Ki of 5.3 and 2.5 nM, potently blocks cAMP formation with IC50 of 16.2 nM.
T12520 Pomaglumetad methionil

LY2140023 hydrate

GluR Neuroscience
Pomaglumetad methionil is an oral methionine prodrug of the potent specific agonist of mGlu2/3 receptor LY404039.
T70619 LY2934747

LY2934747 is a novel, potent, and systemically bioavailable mGlu2/3 receptor agonist, exhibiting both antipsychotic and analgesic properties in vivo.
T38792 LY3027788

LY3027788

LY3027788, a diester analog of LY3020371, an mGlu2/3 receptor antagonist, is a highly potent and orally active prodrug of LY3020371. Notably, LY3027788 exhibits significant antidepressant efficacy.
T78094 Eglumegad hydrochloride

LY354740 hydrochloride,Eglumetad hydrochloride

Eglumegad (LY354740) hydrochloride是一种高效且选择性的group II (mGlu2/3) receptor激动剂,其对人mGlu2mGlu3受体的IC50值分别是5和24 nM。该化合物能够保护神经元不受NMDA毒性影响,并表现出抗焦虑及抗精神病样作用。
T62756 LY487379

LY487379是一种选择性的人类 mGluR2 阳性异生调节剂(PAM)。LY487379 可提高谷氨酸刺激的 [35 S] GTPγS 结合,作用于 mGlu2 受体 (EC50: 1.7 μM) 和 mGlu3 受体 (EC50>10 μM)。LY487379 在大鼠模型中促使认知的灵活性,并诱导行为抑制。LY487379 能够用于研究精神分裂症。
T11906 LY 541850

GluR Neuroscience
LY541850 is a selective orthosteric mGlu2 agonist and mGlu3 antagonist with IC50 values of 0.161 μM and 0.038 μM, respectively.LY 541850 is claimed from human ionotropic and metabotropic glutamate (mGlu) receptors expressed in non-neuronal cells.
T38790 LY3027788 hydrochloride

LY3027788 hydrochloride is a diester analog of LY3020371, a selective antagonist of the metabotropic glutamate 2 and 3 receptors (mGlu2/3). It serves as a highly potent and orally bioavailable prodrug of LY3020371. Notably, LY3027788 hydrochloride exhibits antidepressant efficacy.
T71764 YM 298198 Hydrochloride

YM 298198 Hydrochloride is a non-competitive antagonist with high affinity and selectivity for mGlu1 receptors (Ki = 19 nM). YM 298198 Hydrochloride is inactive at other mGlu receptor subtypes (mGlu2-7), ionotropic receptors and glutamate transporters (IC50 > 10 μM). It inhibits glutamate-induced IP production more potently than CPCCOEt (IC50 values are 16 nM and 6.3 μM respectively).
T71262 AZD-8418

AZD-8418 is an mGlu2 receptor positive allosteric modulators that attenuates nicotine-taking and nicotine-seeking behavior. Acute treatment with AZD8418 (0.37, 1.12, 3.73, 7.46, and 14.92 mg/kg) and AZD8529 (1.75, 5.83, 17.5, and 58.3 mg/kg) deceased nicotine self-administration and had no effect on food-maintained responding. Chronic treatment with AZD8418 attenuated nicotine self-administration, but tolerance to this effect developed quickly. The inhibition of nicotine self-administration by c...

化合物

LY2979165
Cat.No: T15812
Synonym: mGlu2 agonist
Target: GluR
LY404039
Cat.No: T6022
Synonym: pomaglumetad
Target: Glucocorticoid Receptor, GluR
JNJ-42153605
Cat.No: T3451
Synonym:
Target: GluR
MNI 137
Cat.No: T23010
Synonym:
Target: Others, GluR
CBiPES hydrochloride
Cat.No: T22638
Synonym: CBiPES HCl
Target: GluR
Cloransulam-methyl
Cat.No: T20941
Synonym: Cloransulam methyl
Target: Others
ML289
Cat.No: T23000
Synonym: VU0463597,ML 289
Target: GluR
Pomaglumetad methionil hydrochloride
Cat.No: T61972
Synonym: LY2140023 hydrochloride
Target: GluR
VU0361737
Cat.No: T6726
Synonym: ML-128,VU 0361737
Target: GluR
JNJ-40411813
Cat.No: TQ0094
Synonym: ADX-71149
Target: GluR
TASP0433864
Cat.No: T28928
Synonym:
Target:
Ro 64-5229
Cat.No: T23247
Synonym:
Target: Others
JNJ-46356479
Cat.No: T27686
Synonym: JNJ 46356479
Target:
LY2812223
Cat.No: T15809
Synonym:
Target: LIM Kinase
Eglumegad
Cat.No: T15817
Synonym: Eglumetad,LY354740
Target: Others
LY487379 hydrochloride
Cat.No: T22955
Synonym: LY 487379 hydrochloride
Target: Others
VU6001966
Cat.No: T29142
Synonym: VU 6001966,VU-6001966
Target:
VU6001192
Cat.No: T29141
Synonym: VU 6001192,VU-6001192
Target:
RO5488608
Cat.No: T34376
Synonym: RO 5488608,RO-5488608
Target:
LY389795
Cat.No: T27950
Synonym: LY-389795,LY 389795
Target:
JNJ-40068782
Cat.No: T27680
Synonym: JNJ 40068782
Target:
LY3020371 hydrochloride
Cat.No: T11911
Synonym:
Target: GluR
Pomaglumetad methionil
Cat.No: T12520
Synonym: LY2140023 hydrate
Target: GluR
LY2934747
Cat.No: T70619
Synonym:
Target:
LY3027788
Cat.No: T38792
Synonym: LY3027788
Target:
Eglumegad hydrochloride
Cat.No: T78094
Synonym: LY354740 hydrochloride,Eglumetad hydrochloride
Target:
LY487379
Cat.No: T62756
Synonym:
Target:
LY 541850
Cat.No: T11906
Synonym:
Target: GluR
LY3027788 hydrochloride
Cat.No: T38790
Synonym:
Target:
YM 298198 Hydrochloride
Cat.No: T71764
Synonym:
Target:
AZD-8418
Cat.No: T71262
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T3010 Xanthurenic Acid

8-Hydroxykynurenic acid,黄尿酸,4,8-Dihydroxyquinaldic acid,xanthurenate

Apoptosis; Endogenous Metabolite; GluR Apoptosis; Metabolism; Neuroscience
Xanthurenic Acid (8-Hydroxykynurenic acid) 是通过 3-羟基犬尿氨酸转氨而由色氨酸代谢产生的分子,可激活 mGlu2/3 代谢型谷氨酸受体。在下丘脑的感觉传输过程中,它被认为是Group II 代谢型谷氨酸受体的激动剂。

天然产物

Xanthurenic Acid
Cat.No: T3010
Synonym: 8-Hydroxykynurenic acid,黄尿酸,4,8-Dihydroxyquinaldic acid,xanthurenate
Target: Apoptosis, Endogenous Metabolite, GluR
TargetMol Loading
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