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Search Results for " forskolin "

37

抑制剂 & 化合物

6

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T24365	L 858051 7B-Forskolin,L858051,Dmpb-forskolin,L-858051
	L 858051 activates adenylate cyclase. It also inhibits glucose transport in rat adipocytes.
T22467	1,9-Dideoxyforskolin	Others	Others
	The compound is an inactive analog of forskolin(an adenylyl cyclase activator).
T36720	Deacetylforskolin
	Deacetylforskolin is a diterpene and a derivative of forskolin that has been found inC. forskohliiand has diverse biological activities.1,2,3,4It activates rat adipocyte adenylyl cyclase (IC50= 20 μM) and inhibits glucose transport in rat adipocyte plasma membranes.2Deactylforskolin (30-1,000 μg/kg) reduces blood pressure in spontaneously hypertensive rats.3It also attenuates hypercapnia-induced impairments in the passive avoidance response in mice.4 1.Gabetta, B., Zini, G., and Danieli, B.Minor...
T16516	PG01 Phenylglycine-01	CFTR	Membrane transporter/Ion channel
	PG01是一种有效的CFTR Cl-通道增效剂,PG01对 ΔF508（Ka 为 0.3 μM）有效。PG01 对 E193K，G970R 和 G551D (CFTR 突变体)也有效，Kd 值分别为 0.22 μM，0.45 μM 和 1.94 μM 。PG01在加入Forskolin 后可增加ΔF508-CFTR Cl-电流，纠正CFTR 突变体的门控缺陷。
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)。
TP1922L1	ELA-11 (human) acetate(1784687-32-6 free base)	Apelin receptor; Arrestin	GPCR/G Protein
	ELA-11 (human) acetate(1784687-32-6 free base)是亲和力 apelin 受体激动剂 (Ki = 14 nM)。 ELA-32 的生物活性片段。在体外抑制毛喉素诱导的 cAMP 产生并刺激 β-arrestin 募集。
T39392L	C-Type Natriuretic Peptide (CNP) (1-22), human acetate C-Type Natriuretic Peptide (CNP) (1-22), human acetate(1966153-17-2 Free base)	Others	Others
	C-Type Natriuretic Peptide (CNP) (1-22), human acetate 是一种利钠肽受体 B (NPR-B) 的激动剂，一种内皮衍生的松弛剂和生长抑制因子。 C-Type Natriuretic Peptide (CNP) (1-22), human acetate 抑制由组胺和 5-HT 或直接由毛喉素刺激的 cAMP 合成。
TP1936L1	RFRP3(human) acetate(311309-27-0 free base)	Neuropeptide Y Receptor	GPCR/G Protein; Neuroscience
	RFRP3(human) acetate(311309-27-0 free base) 是一种人类 GnIH 肽同源物，是一种有效的促性腺激素分泌抑制剂，可抑制 Ca2+ 动员。它是一种 NPFF1 受体激动剂，它抑制毛喉素诱导的 cAMP 产生，IC50 为 0.7 nM。
TP1187	C-Type Natriuretic Peptide (CNP) (1-22), human CNP (1-22), human	RAAS	Endocrinology/Hormones
	C-Type Natriuretic Peptide (CNP) (1-22), human 是一种利钠肽受体 B (NPR-B) 激动剂，是一种 CNP 的 1-22 片段。它对生理激动剂组胺和 5-HT 刺激或直接由 Forskolin 刺激的 cAMP 合成具有抑制作用。其中CNP 是一种有效的、内皮衍生的松弛剂和生长抑制因子。
T10591L	(R)-BPO-27	CFTR; Autophagy	Autophagy; Membrane transporter/Ion channel
	(R)-BPO-27 是一种具有口服活性和高效性的 ATP 竞争性 CFTR 抑制剂(IC50：4 nM)，可用于研究腹泻和多囊肾。
T33214	Manoyl oxide Manoyl
	Manoyl oxide is a proposed intermediate in the biosynthesis of forskolin and other medically important labdane-type terpenoids.
T27779	L-759,656 L 759,656,L759,656
	L-759,656 is highly selective CB2 receptor agonist (CB1 Ki = 4888 nM, CB2 Ki = 11.8 nM). L-759,656 potently inhibits forskolin-stimulated cAMP production in CHO cells (EC50 = 3.1 nM).
TP1922	ELA-11(human) ELA-11 (human)
	High affinity apelin receptor agonist (Ki = 14 nM). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.
T76053	ELA-11(human) TFA
	ELA-11(human) TFA is a high affinityapelin receptoragonist (Ki=14 nM). ELA-11(human) TFA is a bioactive fragment of ELA-32. ELA-11(human) TFA inhibits forskolin-induced cAMP production and stimulates β-arrestin recruitment in vitro.
T39442	AM-8123
	AM-8123 is an APJ agonist with high oral bioavailability and potency. It effectively inhibits Forskolin-stimulated cAMP production and activates Gα proteins. This compound is valuable for cardiovascular disease research.
T78083	CB-25	Cannabinoid Receptor	GPCR/G Protein
	CB-25是一种CB1大麻素受体的部分激动剂配体。它能增强Forskolin诱导的癌细胞中cAMP的形成，但在Forskolin诱导的hCB1-CHO细胞中则不显示增强作用。
TP2092	Apelin-17(human, bovine) Apelin-17 (human, bovine)
	Endogenous apelin receptor agonist. Potently inhibits forskolin-stimulated cAMP accumulation (pIC50 = 9.94).
TP2096	ELA-21 (human)
	High affinity apelin receptor agonist. Binds apelin receptors in left ventricle from normal and pulmonary arterial hypertensive (PAH) hearts (pKi values are 9.31 and 9.46, respectively). Bioactive fragment of ELA-32. Inhibits forskolin-induced cAMP produc
TP1936	RFRP-3(human) RFRP 3 (human)
	Agonist of the NPFF1 receptor (IC50 = 0.7 nM for inhibition of forskolin-induced cAMP production). Homolog of gonadotropin-inhibitory hormone (GnIH); inhibits activity of gonadotropin-releasing hormone (GnRH) neurons.
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
T75866	RFRP-3(human) TFA
	RFRP-3 (Neuropeptide VF(124-131))(human) TFA，一种人 GnIH 肽同源物，是一种促性腺激素分泌抑制 Ca2+动员的有效抑制剂。RFRP-3(human) TFA 是一种NPFF1受体激动剂，它抑制 forskolin 诱导的 cAMP 生成的 IC50值为 0.7 nM。
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。
T39392	C-Type Natriuretic Peptide (CNP) (1-22), human TFA
	C-Type Natriuretic Peptide (CNP) (1-22), human (TFA), is a 22 amino acid fragment of CNP and functions as an agonist for the natriuretic peptide receptor B (NPR-B). It can inhibit cAMP synthesis, which is induced by histamine, 5-HT, or Forskolin. Additionally, CNP exhibits strong endothelial-derived relaxation properties and acts as a growth inhibitor.
T37477	L-858,051 (hydrochloride)
	L-858,051 is a water-soluble analog of forskolin , a cell-permeant activator of adenylate cyclase. L-858,051 activates adenylate cyclase (EC50 = 3 μM), inhibits glucose transport, and blocks cytochalasin B binding in rat adipocyte membranes. L-858,051 is used to activate adenylate cyclase and initiate signaling through elevated cAMP synthesis in a variety of cell types in culture.
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...
T37896	AZ 1729
	FFA2 allosteric agonist. Inhibits forskolin-induced cAMP increase and stimulates 35SGTPγS binding in biochemical assays (pEC50 values are 6.9 and 7.23, respectively). Binds at allosteric binding site. In functional assays, displays positive allosteric modulation of FFA-induced Gi signaling and negative allosteric modulation of FFA-induced Gq/G11 signaling. Inhibits lipolytic effect of isoproterenol (pEC50 = 5.03) and induces migration of human neutrophils in vitro. Bolognini et al (2016) A novel...
T37131	MS 15203
	Potent and selective GPR171 partial agonist (EC50 = 90 nM; 28% inhibition of forskolin activated adenylyl cyclase activity in rat hypothalamic memebranes). Exhibits minimal binding to a panel of ~70 GPCRs and 10 other receptors (<22% of radioligand displaced from the target receptors). Increases neuronal activity in the paraventricular nucleus. Increases food intake and body weight in mice. Wardman et al (2016) Identification of a small-molecule ligand that activates the neuropeptide receptor GP...
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...
T69537	Difelikefalin HCl
	Difelikefalin HCl is a κ-opioid receptor (KOR) agonist. It activates KOR in HEK293 cells expressing the human receptor (EC50 = 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50 = 0.048 nM). Difelikefalin HCl is selective for KOR over the μ-opioid receptor (MOR; EC50 = >1 µM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07...
T37483	Difelikefalin (trifluoroacetate salt)
	Difelikefalin is a κ-opioid receptor (KOR) agonist.1It activates KOR in HEK293 cells expressing the human receptor (EC50= 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50= 0.048 nM). Difelikefalin is selective for KOR over the μ-opioid receptor (MOR; EC50= >1 μM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 m...
T69530	Difelikefalin TFA
	Difelikefalin TFA is a κ-opioid receptor (KOR) agonist. It activates KOR in HEK293 cells expressing the human receptor (EC50 = 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50 = 0.048 nM). Difelikefalin TFA is selective for KOR over the μ-opioid receptor (MOR; EC50 = >1 µM in a transactivation assay). It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07...
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...
T83955	MOMBA
	MOMBA是一种针对人类自由脂肪酸2(hFFA2)工程化受体和设计药物激活的设计受体(DREADD)的选择性正交激动剂，对野生型hFFA2、hFFA3和小鼠FFA2无活性。MOMBA能够在表达hFFA2-DREADD受体的细胞中抑制forskolin刺激的cAMP水平，其功效改善且与山梨酸的效力相当。在hFFA2-DREADD转基因小鼠中，MOMBA治疗显著降低肠道传输速度，并促进依赖浓度的结肠隐窝GLP-1释放。该化合物具有口服生物利用度。
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。
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。
T37791	A-971432
	A-971432 is a sphingosine-1-phosphate receptor 5 (S1P5) agonist that is selective for S1P5 over S1P1 and S1P3 (IC50s = 0.006, 0.362, and >10 &#181M, respectively). It inhibits forskolin-induced cAMP production in CHO cells expressing S1P5 (EC50 = 4.1 nM). A-971432 (1 &#181M) increases electrical resistance of hCMEC/D3 cells in an in vitro blood-brain barrier model, indicating enhanced barrier integrity, and attenuates blood-brain barrier leakage in an R6/2 transgenic mouse model of Huntington’s ...
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: T24365

Synonym: 7B-Forskolin,L858051,Dmpb-forskolin,L-858051

1,9-Dideoxyforskolin

Cat.No: T22467

Target: Others

Deacetylforskolin

Cat.No: T36720

Cat.No: T16516

Synonym: Phenylglycine-01

Target: CFTR

Apelin-17 (human, bovine) acetate

Cat.No: TP2092L

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

Target: HIV Protease

ELA-11 (human) acetate(1784687-32-6 free base)

Cat.No: TP1922L1

Target: Apelin receptor, Arrestin

C-Type Natriuretic Peptide (CNP) (1-22), human acetate

Cat.No: T39392L

Synonym: C-Type Natriuretic Peptide (CNP) (1-22), human acetate(1966153-17-2 Free base)

Target: Others

RFRP3(human) acetate(311309-27-0 free base)

Cat.No: TP1936L1

Target: Neuropeptide Y Receptor

C-Type Natriuretic Peptide (CNP) (1-22), human

Cat.No: TP1187

Synonym: CNP (1-22), human

Target: RAAS

Cat.No: T10591L

Target: CFTR, Autophagy

Cat.No: T33214

Synonym: Manoyl

Cat.No: T27779

Synonym: L 759,656,L759,656

Cat.No: TP1922

Synonym: ELA-11 (human)

ELA-11(human) TFA

Cat.No: T76053

Cat.No: T39442

Cat.No: T78083

Target: Cannabinoid Receptor

Apelin-17(human, bovine)

Cat.No: TP2092

Synonym: Apelin-17 (human, bovine)

Cat.No: TP2096

Cat.No: TP1936

Synonym: RFRP 3 (human)

Cat.No: TP2001

RFRP-3(human) TFA

Cat.No: T75866

Cat.No: T78949

Target: Cannabinoid Receptor

C-Type Natriuretic Peptide (CNP) (1-22), human TFA

Cat.No: T39392

L-858,051 (hydrochloride)

Cat.No: T37477

Peptide YY (human) (trifluoroacetate salt)

Cat.No: T35631

Synonym: Peptide Tyrosine Tyrosine

Cat.No: T37896

Cat.No: T37131

Cat.No: T37199

Difelikefalin HCl

Cat.No: T69537

Difelikefalin (trifluoroacetate salt)

Cat.No: T37483

Difelikefalin TFA

Cat.No: T69530

Cat.No: T70035

Cat.No: T83955

Neuropeptide Y (porcine, bovine) TFA

Cat.No: T83677

Synonym: NPY (porcine, bovine)

Galanin (Human) (Acetate)

Cat.No: T38110

Cat.No: T37791

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
T2939	Forskolin 毛喉素,Coleonol,Colforsin	FXR; Adenylyl cyclase; AChR; Autophagy	Autophagy; Metabolism; Neuroscience
	Forskolin (Coleonol) 属于天然产物，是一种腺苷酸环化酶激活剂 (EC50=0.5 μM)。Forskolin 可以增加 cAMP 水平，可以激活 PXR 和 FXR，也可以诱导细胞自噬。Forskolin 对心脏产生正性肌力作用，具有血小板抗凝集和降压作用。
TN4073	Forskolin G	Others	Others
	Forskolin is known to elevate intracellular cAMP levels.
TN4074	Forskolin J	Others	Others
	Forskolin J 是一种天然产物，可用于生命科学领域的相关研究。其产品编号为 TN4074，CAS号为 81873-08-7。
TN1520	Isoforskolin Coleonol B	IL Receptor; TNF	Apoptosis; Immunology/Inflammation
	Isoforskolin 源自毛喉鞘蕊花，可减少人单核白细胞中 TNF-α、IL-1β、IL-6 和 IL-8 的分泌。Isoforskolin 可用于治疗莱姆关节炎的研究。
T5081	Adenine monohydrochloride hemihydrate 腺嘌呤盐酸盐,Adenine hydrochloride hydrate,6-Aminopurine hydrochloride hydrate	Endogenous Metabolite; Adenosine Receptor	GPCR/G Protein; Metabolism; Neuroscience
	Adenine monohydrochloride hemihydrate 是内源性代谢产物的一种。
T16332	NKH477 Colforsin dapropate hydrochloride	NMDAR	Neuroscience
	NKH477 is a novel water-soluble forskolin derivative that improves cardiac failure mainly through its beneficial effects on diastolic cardiac function. NKH477 shows an antiproliferative effect in vivo with an altered cytokine profile to inhibit the acute

天然产物

Cat.No: T2939

Synonym: 毛喉素,Coleonol,Colforsin

Target: FXR, Adenylyl cyclase, AChR, Autophagy

Cat.No: TN4073

Target: Others

Cat.No: TN4074

Target: Others

Cat.No: TN1520

Synonym: Coleonol B

Target: IL Receptor, TNF

Adenine monohydrochloride hemihydrate

Cat.No: T5081

Synonym: 腺嘌呤盐酸盐,Adenine hydrochloride hydrate,6-Aminopurine hydrochloride hydrate

Target: Endogenous Metabolite, Adenosine Receptor

Cat.No: T16332

Synonym: Colforsin dapropate hydrochloride

Target: NMDAR

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