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Search Results for " camp accumulation "

32

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9238	KI-7	Adenosine Receptor	GPCR/G Protein; Neuroscience
	KI-7 是一种A2B 腺苷受体阳性变构调节剂。它增强选择性 A2B 腺苷受体激动剂 BAY 60-6583 和腺苷诱导的 cAMP 积累，EC50分别为 2390 nM 和 2550 nM。它也增强非选择性 A2B 腺苷受体激动剂 NECA 诱导的 cAMP 积累，EC50为 445.8 nM。
T3478	Ro 67-7476	GluR	Neuroscience
	Ro 67-7476 是mGluR1的正变位调节剂，能增强表达 rat mGluR1a 的 HEK293 细胞中谷氨酸诱导的钙释放，EC50为 60.1 nM。它是 P-ERK1/2 激动剂，可以在外源添加谷氨酸的情况下激活 ERK1/2 磷酸化 (EC50=163.3 nM)。
TP2092L	Apelin-17 (human, bovine) acetate Apelin-17 (human, bovine) acetate(217082-57-0 free base)	HIV Protease	Microbiology/Virology; Proteases/Proteasome
	Apelin-17 (human, bovine) acetate(217082-57-0 free base) 是一种内源性 apelin 受体激动剂。有效抑制毛喉素刺激的 cAMP 积累 (pIC50 = 9.94)。
TP2009L	K 41498 aceate	CRFR	GPCR/G Protein
	K41498 acetate 是 antisauvagine-30 的类似物，可抑制 suvagine 刺激的 cAMP 在表达 hCRF2α 和 hCRF2β 的细胞中的积累。 K41498 acetate 是一种有效且高度选择性的 CRF2 受体拮抗剂，对人 CRF2α、CRF2β 和 CRF1 受体的 Ki 值分别为 0.66 nM、0.62 nM 和 425 nM。
T12913	Siguazodan SKF 94836	PDE	Metabolism
	Siguazodan (SKF 94836) 是选择性的，口服有效的磷酸二酯酶 III 抑制剂，IC50为 117 nM。它可增加完整血小板中 cAMP 的积累，EC50为 18.88 μM。它也抑制苯肾上腺素诱导的 5-HT 释放，IC50为 4.2 μM。
T12970	Solabegron GW 427353,3'-[[2-[(2R)-2-(3-氯苯基)-2-羟基乙基]氨基]乙基]氨基]-[1,1'-联苯基]-3-羧酸	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Solabegron (GW 427353) 是一种β3肾上腺素能受体 (β3-AR)的选择性激动剂, 在中国仓鼠卵巢细胞中测得 EC50=22 nM，可用于研究膀胱过度活跃和肠易激综合征。
T23581	2-Methylthioadenosine diphosphate trisodium 2 Methylthio ADP,2MeSADP,2-Methylthio-ADP,2 MeS ADP,2-MeS-ADP
	2-MeS-ADP is a purinergic agonist that acts by displaying selectivity for P2Y1, P2Y12, and P2Y13 receptors and inhibiting cAMP accumulation.
TP2092	Apelin-17(human, bovine) Apelin-17 (human, bovine)
	Endogenous apelin receptor agonist. Potently inhibits forskolin-stimulated cAMP accumulation (pIC50 = 9.94).
TP2021	[Pro3]-GIP (Rat)
	High affinity rat GIP receptor partial agonist (Kd = 13 nM). Increases cAMP accumulation in COS-7 cells transfected with rat GIP receptor, while also acting as a competitive antagonist of GIP.
TP2001	MM 54
	Potent apelin receptor antagonist (Ki = 82 nM; IC50 = 93 nM). Antagonizes the inhibitory affect of [Pyr1]-Apelin-13 on forskolin-induced cAMP accumulation in CHO-K1-APJ cells. Recuces tumor expansion and lengthens survival time in a mouse xenograft model
TP2009	K41498 K 41498
	Potent and highly selective CRF2 receptor antagonist (Ki values are 0.66, 0.62 and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively). Inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. In rats in vivo, blo
T83743	VPM-p15 TFA T1V/F3Phe(4-Me)
	VPM-p15是一种合成多肽激动剂，针对粘附G蛋白偶联受体(GPCR) G2 (ADGRG2)而设计，ADGRG2是一种孤儿GPCR，与男性不育有关。在表达人类ADGRG2的HEK293细胞中，它能诱导cAMP积累（EC50 = 1.41 µM）。
T78949	AM841	Cannabinoid Receptor	GPCR/G Protein
	AM841是一种高亲和力的亲电子配体，能与CB1大麻素受体中第六螺旋的半胱氨酸发生共价作用并激活该受体。此外，AM841能减少Forskolin刺激下的cAMP积累，并且减缓胃肠蠕动。
T36634	ZQ 16
	Selective medium-chain free fatty acid receptor GPR84 agonist (EC50 = 139 nM). Exhibits no response at GPR40, GPR41, GPR119 or GPR120 at 100 μM. Activates calcium mobilization, inhibits cAMP accumulation, and induces ERK1/2 phosphorylation, receptor desensitization and internalization in vitro. Liu et al (2016) Design and synthesis of 2-alkylpyrimidine-4,6-diol and 6-alkylpyridine-2,4-diol as potent GPR84 agonists. ACS Med.Chem.Lett. 7 579 PMID:27326330 \|Zhang et al (2016) Discovery and characte...
TP2091	Antisauvagine-30
	Potent, selective and competitive corticotropin-releasing factor CRF2 receptor antagonist (Kd values are 1.4 and 153.6 nM for binding to mouse CRF2β and rat CRF1 receptors respectively). Inhibits sauvagine-stimulated cAMP accumulation in HEK-mCRF2β cells
T79913	GRK2 Inhibitor 2
	GRK2 Inhibitor 2 (Compound 8h) 作为一种高效的抑制剂，对GRK2有显著的抑制活性（IC50: 19 nM），同样对Aurora-A也表现出抑制作用（IC50: 137 nM）。该化合物能增强GRK2过表达的HEK293细胞中β-AR介导的cAMP积累。此外，GRK2 Inhibitor 2适用于充血性心力衰竭（HF）的相关研究。
TP2071	Bay 55-9837
	Selective VPAC2 receptor agonist (EC50 values are 0.4, 100 and >1000 nM for VPAC2, VPAC1 and PAC1, respectively in a cAMP accumulation assay; IC50 values are 60, 8700 and >10000 nM for VPAC2, VPAC1 and PAC1, respectively in a competition binding assay). S
T69824	PSB-17365
	PSB-17365 is a potent GPR84 agonist. PSB-17365 exhibits EC50 values vs. GPR84 of 2.5nM in a cAMP accumulation assay, and 100nM in a β-arrestin 2 recruitment assay. No direct binding affinities are provided. PSB-17365 is selective for GPR84 compared to other free fatty acid receptors (FFAR1 and FFAR4). GPR84, a Gi protein-coupled receptor that is activated by medium-chain (hydroxy)fatty acids, appears to play an important role in inflammation, immunity, and cancer.
T37199	Bilaid C
	Bilaid C is a tetrapeptide μ-opioid receptor agonist (Ki= 210 nM in HEK293 cell membranes expressing the human receptor) that has been found inPenicillium.1It inhibits forskolin-induced cAMP accumulation by 77% in HEK293 cells expressing the human μ-opioid receptor when used at a concentration of 10 μM. Bilaid C induces inward rectifying potassium channel (Kir) currents in rat locus coeruleus slices that endogenously express high levels of the μ-opioid receptor (EC50= 4.2 μM). 1.Dekan, Z., Siana...
T70035	Tasimelteon-d5
	Tasimelteon-d5 is intended for use as an internal standard for the quantification of tasimelteon by GC- or LC-MS. Tasimelteon is a melatonin (MT) receptor agonist. It selectively binds MT1 and MT2 receptors over a panel of 160 additional receptors and enzymes at 10 µM. Tasimelteon inhibits forskolin-induced cAMP accumulation with EC50 values of 0.79 and 1 nM in NIH3T3 cells expressing the MT1 or MT2 receptor, respectively. Formulations containing tasimelteon have been used in the treatment of no...
T35631	Peptide YY (human) (trifluoroacetate salt) Peptide Tyrosine Tyrosine
	Peptide YY (PYY) is a 36-amino acid peptide and anorectic gut hormone agonist for the neuropeptide Y receptors Y1, Y2, Y5, and Y6 with EC50 values of 0.7, 0.58, 1, and 0.8 nM, respectively, for supression of forskolin-induced cAMP accumulation. PYY is cleaved in vivo to PYY (3-36) . Release of PYY occurs postprandially in proportion to calorie intake from intestinal enteroendocrine L cells, indicating it may be a satiety signal. In humans, PYY inhibits food intake and gastrointestinal transit in...
T75804	K41498 TFA
	K41498 TFA 是一种强选择性的CRF2 receptor 拮抗剂，其对人 CRF2α、CRF2β和 CRF1受体的Ki 值分别为 0.66 nM、0.62 nM 和425 nM。K41498 TFA 是 antisauvagine-30 (aSvg-30) 的类似物，可抑制 sauvagine 刺激的 cAMP 在 hCRF2α/hCRF2β表达细胞中的积累。K41498 可用于低血压研究。
T83178	ACTH (6-24) (human) Adrenocorticotropic hormone (6-24)
	ACTH (6-24) (human)（腎上腺皮質激素（6-24））是腎上腺皮質激素的片段。該化合物作為ACTH (1-39) 和 ACTH (5-24) 引起的類固醇生成的競爭性抑制劑，具有相應的Kd值分別為13.4和3.4nM。此外，ACTH (6-24) (human) 能夠抑制 hPTH 1-34 所誘導的皮質酮產生以及cAMP的累積。
T36555	Tyr-α-CGRP (human) (trifluoroacetate salt)
	Tyr-α-CGRP is an N-terminal extended tyrosinated analogue of α-calcitonin gene-related peptide . It binds to amylin receptors AMY1 and AMY3 in COS-7 cells expressing the human receptors (IC50s = 141 and 1.86 nM, respectively). Tyr-α-CGRP also binds to and stimulates cAMP accumulation in rat L6 myocytes (IC50 = 4 nM; EC50 = 12 nM). It also binds to rat brain and spleen membrane preparations (IC50s = 0.2 and 0.5 nM, respectively), induces positive chronotropic and inotropic effects in isolated rig...
T36427	PACAP (6-27) (human, chicken, mouse, ovine, porcine, rat) (trifluoroacetate salt)	PACAP	GPCR/G Protein
	Pituitary adenylate cyclase-activating peptide (PACAP) (6-27) is a PACAP receptor antagonist with IC50 values of 1,500, 600, and 300 nM, respectively, for rat PAC1, rat VPAC1, and human VPAC2 recombinant receptors expressed in CHO cells. It binds to PACAP receptors on SH-SY5Y and SK-N-MC human neuroblastoma and T47D human breast cancer cells (IC50s = 24.5, 106, and 105 nM, respectively) and inhibits cAMP accumulation induced by PACAP (1-38) (Kis = 457, 102, and 283 nM, respectively, in SH-SY5Y, ...
T38110	Galanin (Human) (Acetate)
	Galanin (Human) (Acetate)是一种含有30个氨基酸的神经肽和丙氨酸(GAL)受体激动剂。在表达重组人gal1受体的HEK293E 细胞(EC50= 0.031 nM)中，它抑制佛司可林诱导的cAMP 产生，并刺激表达重组人gal2受体的CHO 细胞(EC50= 12.3 nM)中肌醇磷酸的积累。Galanin (Human) (Acetate)诱导离体大鼠纵向眼底收缩，ec50值为13.8 nM。在大鼠福尔马林试验的第二阶段，鞘内给药人甘丙肽(3、10和30 nmol/只)可减少大鼠舔爪和退缩。
T37354	CAY10680 CAY10680
	CAY10680 is a dopamine-sparing, benzothiazinone compound that selectively inhibits both MAO-B activity (IC50 = 34.9 nM in human) and adenosine A2A receptors (Ki = 39.5 nM in human). It demonstrates significantly less potent inhibitory values for other adenosine receptor subtypes (Kis > 1 μM) and MAO-A (IC50 ≥ 10 μM). At 1-20 μM, CAY10680 has been shown to abolish cAMP accumulation in CHO cells transfected with adenosine A2A receptors. In the central nervous system adenosine A2A receptor expressi...
T35573	Adenosine 5’-methylenediphosphate (hydrate)
	Adenosine 5’-methylenediphosphate is an inhibitor of ecto-5’-nucleotidase, also known as CD73, with a Kivalue of 37 nM.1It inhibits cAMP accumulation induced by adenosine 5’-monophosphate , adenosine 5’-diphosphate , or adenosine 5’-triphosphate but not adenosine in VA-13 human fibroblasts when used at a concentration of 100 μM. Adenosine 5’-methylenediphosphate reduces proliferation of U138MG glioma cells, as well as inhibits the invasion and migration of MHCC97H hepatocellular carcinoma (HCC) ...
T37413	Calcitonin (salmon) (trifluoroacetate salt)
	Calcitonin is a peptide hormone that lowers blood calcium level and inhibits bone resorption. It belongs to the calcitonin family of peptides, which also includes amylin , calcitonin gene-related peptide , and adrenomedullin. The binding of salmon calcitonin to the human calcitonin receptor (CTR) is not modulated by receptor activity-modifying proteins (RAMPs), which influence affinity of human calcitonin to CTR. Salmon calcitonin binds to human CTR2 with IC50 values of 0.933, 0.224, 0.134, and ...
T83677	Neuropeptide Y (porcine, bovine) TFA NPY (porcine, bovine)
	神经肽Y（Neuropeptide Y, NPY）是一种参与调节食欲、血管收缩、心脏收缩力和肠道分泌的神经肽，同时也是NPY受体Y1、Y2和Y5的激动剂。它在全身范围内表达。NPY能够在表达大鼠Y1或Y2以及表达大鼠Y5的HEK293细胞中选择性抑制由forskolin诱导的cAMP积累，而对表达大鼠Y4受体的L-M(TK-)细胞的影响较小（EC50分别为0.15、2.7、0.66和>1,000 nM)。在分离的豚鼠心脏模型中，NPY能够增加灌注压（EC30 = 1.3 nM）。神经内注射NPY（300 pmol/动物）能够在大鼠中增加食物摄取量。
T75909	[Nphe1]Nociceptin(1-13)NH2 TFA
	[Nphe1]Nociceptin(1-13) NH2 TFA 是一种 Nociceptin/orphanin FQ (NC)内源性配体，是一种选择性和竞争性的 ociceptin receptor 拮抗剂，不具有激动剂活性。[Nphe1]nociceptin(1-13)NH2 选择性结合重组 nociceptin 受体(pKi=8.4)，拮抗 nociceptin 对 CHO 细胞中 cAMP 积累的抑制作用(pA2=6.0)。[Nphe1]Nociceptin(1-13)NH2 有可能作为一种止痛试剂。
T83697	PAMP-12 (human, mouse, rat, porcine, bovine) TFA Proadrenomedullin N-terminal 12 Peptide,PAMP (9-20)
	Proadrenomedullin N-terminal 12 peptide (PAMP-12) 是一种内源性肽段，源自人体肾上腺髓质，对应人类PAMP-20的9-20氨基酸，涉及降低血压。它是MAS相关G蛋白偶联受体家族成员X2 (MRGPRX2) 的激动剂。在表达人MRGPRX2的CHO细胞中，PAMP-12抑制forskolin诱导的cAMP积累（EC50 = 57.2 nM），特异性诱导表达MRGPRX2的CHO细胞的钙离子动员（EC50 = 41 nM），而在表达MRGPRX1、MRGPRX3或MRGPRX4的细胞中则无此效应（在1 µM浓度下）。PAMP-12还能作为烟碱型乙酰胆碱受体（nAChRs）的拮抗剂，抑制carbachol诱导的儿茶酚胺释放（IC50 = 1.3 µM）及钙和钠的流入（IC50分别为0.39 µM和0.87 µM），但不抑制组胺诱导的儿茶酚胺释放或钙和钠的流入（IC50 >1 µM），在初级牛肾上腺嗜铬细胞中有此表现。当以10至50 nmol/kg剂量给予正常血压大鼠时，PAMP-12能降低平均动脉血压。

化合物

Cat.No: T9238

Target: Adenosine Receptor

Cat.No: T3478

Target: GluR

Apelin-17 (human, bovine) acetate

Cat.No: TP2092L

Synonym: Apelin-17 (human, bovine) acetate(217082-57-0 free base)

Target: HIV Protease

Cat.No: TP2009L

Target: CRFR

Cat.No: T12913

Synonym: SKF 94836

Target: PDE

Cat.No: T12970

Synonym: GW 427353,3'-[[2-[(2R)-2-(3-氯苯基)-2-羟基乙基]氨基]乙基]氨基]-[1,1'-联苯基]-3-羧酸

Target: Adrenergic Receptor

2-Methylthioadenosine diphosphate trisodium

Cat.No: T23581

Synonym: 2 Methylthio ADP,2MeSADP,2-Methylthio-ADP,2 MeS ADP,2-MeS-ADP

Apelin-17(human, bovine)

Cat.No: TP2092

Synonym: Apelin-17 (human, bovine)

[Pro3]-GIP (Rat)

Cat.No: TP2021

Cat.No: TP2001

Cat.No: TP2009

Synonym: K 41498

Cat.No: T83743

Synonym: T1V/F3Phe(4-Me)

Cat.No: T78949

Target: Cannabinoid Receptor

Cat.No: T36634

Antisauvagine-30

Cat.No: TP2091

GRK2 Inhibitor 2

Cat.No: T79913

Cat.No: TP2071

Cat.No: T69824

Cat.No: T37199

Cat.No: T70035

Peptide YY (human) (trifluoroacetate salt)

Cat.No: T35631

Synonym: Peptide Tyrosine Tyrosine

Cat.No: T75804

ACTH (6-24) (human)

Cat.No: T83178

Synonym: Adrenocorticotropic hormone (6-24)

Tyr-α-CGRP (human) (trifluoroacetate salt)

Cat.No: T36555

PACAP (6-27) (human, chicken, mouse, ovine, porcine, rat) (trifluoroacetate salt)

Cat.No: T36427

Target: PACAP

Galanin (Human) (Acetate)

Cat.No: T38110

Cat.No: T37354

Synonym: CAY10680

Adenosine 5’-methylenediphosphate (hydrate)

Cat.No: T35573

Calcitonin (salmon) (trifluoroacetate salt)

Cat.No: T37413

Neuropeptide Y (porcine, bovine) TFA

Cat.No: T83677

Synonym: NPY (porcine, bovine)

[Nphe1]Nociceptin(1-13)NH2 TFA

Cat.No: T75909

PAMP-12 (human, mouse, rat, porcine, bovine) TFA

Cat.No: T83697

Synonym: Proadrenomedullin N-terminal 12 Peptide,PAMP (9-20)

Cat. No.	Product Name	Target	Signaling Pathways
T1626	Prostaglandin E1 前列地尔,PGE1,列腺素E1,Alprostadil	Endogenous Metabolite; Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation; Metabolism
	Prostaglandin E1 (Alprostadil) 是一种前列腺素受体配体，对小鼠 EP1、EP2、EP3、EP4和 IP 的 Ki 值分别为 36、10、1.1、2.1 和 33 nM。它诱导血管舒张并抑制血小板聚集，可作为血管扩张剂用于外周血管疾病的研究。
T19122	3-Methylvaleric Acid	Others; Endogenous Metabolite	Metabolism; Others
	3-Methylvaleric Acid 是一种食用级香料，存在于烟草中。3-Methylvaleric Acid 可增强 CHO-K1细胞和HEK293细胞中的细胞内cAMP 积累和CRE-荧光素酶活性。

天然产物

Prostaglandin E1

Cat.No: T1626

Synonym: 前列地尔,PGE1,列腺素E1,Alprostadil

Target: Endogenous Metabolite, Prostaglandin Receptor

3-Methylvaleric Acid

Cat.No: T19122

Target: Others, Endogenous Metabolite

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