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Search Results for " human whole blood "

29

抑制剂 & 化合物

3

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T9020	GSK620	Epigenetic Reader Domain	Chromatin/Epigenetic
	GSK620 是一种有口服活性的泛BD2抑制剂，在人全血中表现出抗炎表型，有良好的广谱选择性、可开发性和体内口服药代动力学。它对 BET-BD2 家族蛋白具有高度选择性，其选择性超过所有其他 BET 溴结构域 200 倍以上。
T14975	CJ-42794 CJ-042794	Others	Others
	CJ-42794 (CJ-042794)是前列腺素受体 EP4的选择性拮抗剂, 抑制[3H]-PGE2与 EP4受体结合的平均 pKi 为8.5, 对 EP4选择性比 EP1, EP2和 EP3高200多倍。
T32824	LM-1685 LM 1685,LM1685	COX	Immunology/Inflammation; Neuroscience
	LM-1685是一种有效且具有选择性的人单核细胞和全血中COX-2抑制剂，IC50分别为0.65 µM 和IC50 = 4.3 μM，是治疗炎症的潜在化合物。
T10866	Cot inhibitor-2	TNF; MAPK	Apoptosis; MAPK
	Cot inhibitor-2 是一种 cot (Tpl2/MAP3K8) 抑制剂(IC50 : 1.6 nM)，具有有效性，选择性和口服活性。Cot inhibitor-2 对LPS 刺激的人全血中 TNF-α 的产生具有抑制作用，IC50 为 0.3 μM。
T26531	ABT-963 ABT963
	ABT-963 is a cyclooxygenase 2 (COX-2) inhibitor potentially for the treatment of osteoarthritis and pain. ABT-963 has excellent selectivity in human whole blood, high oral anti-inflammatory potency in vivo, and gastric safety in the animal studies.
T10865L	Cot inhibitor-1 hydrochloride Cot inhibitor-1 hydrochloride(915365-57-0 Free base)	TNF; MAPK	Apoptosis; MAPK
	Cot inhibitor-1 hydrochloride 是肿瘤进展位点 2 激酶 (IC50 = 28 nM) 的抑制剂，可抑制人全血中 TNF-α 的产生 (IC50 = 5.7 nM)。
T68155	Tebufelone	Prostaglandin Receptor; LTR	GPCR/G Protein; Immunology/Inflammation
	Tebufelone 是一种体外高效的CO 抑制剂，是一种新型的非甾体抗炎药（NSAID），属于二叔丁基苯酚（DTBP）类，在各种动物模型中显示出强大的抗炎、镇痛和抗网膜炎特性。Tebufelone 能有效地抑制前列腺素（PGE2）的形成，阻止大鼠巨噬细胞（IC50 = 20 microM）和人类全血（IC50 = 22 microM）中脂氧酶途径的产物[白三烯（LTB4）]的体外形成。
T3631	PF-8380	PDE	Metabolism
	PF8380 是有效的autotaxin 抑制剂，在体外酶实验和人类全血细胞实验中的IC50分别为 2.8 nM 和 101 nM。
T10865	Cot inhibitor-1	TNF; MAPK	Apoptosis; MAPK
	Cot inhibitor-1 是一种选择性的 Cot 蛋白激酶(也被称为 Tpl2或 MAP3K8)抑制剂(IC50 为 28 nM)。Cot inhibitor-1 抑制人全血中 TNF-alpha 的产生，其 IC50 为 5.7 nM。Cot 参与多种细胞信号通路，特别是与炎症和免疫反应有关的信号通路。Cot inhibitor-1抑制 Cot 活性，可能对类风湿关节炎、炎症性肠病和某些类型的癌症具有潜在的治疗效果。
T0463	Loxoprofen Loxoprofene,洛索洛芬,Loxoprofeno,Koloxo	COX	Immunology/Inflammation; Neuroscience
	Loxoprofen (Koloxo) 是一种非甾体类抗炎药，具有解热作用，可用于缓解疼痛的研究。它是非选择性COX 抑制剂，对 COX-1 和 COX-2 的IC50分别为 6.5 和 13.5 μM。
T14374	AZD2906
	AZD2906, a selective glucocorticoid receptor (GR) agonist, demonstrates inhibitory concentrations (IC50s) of 2.2 nM in human GR, 0.3 nM in rat peripheral blood mononuclear cells (PBMC), 41.6 nM in human whole blood, and 7.5 nM in rat whole blood, respectively[1]. Additionally, it induces an increase in micronucleated immature erythrocytes within rat bone marrow.
T14381	AZD7624 AZD-7624	p38 MAPK; TNF	Apoptosis; MAPK
	AZD7624 是一种 p38 抑制剂，具有强大的抗炎活性。
T35725	4-hydroxy Valsartan
	4-hydroxy Valsartan is a major metabolite of the angiotensin II type 1 (AT1) receptor antagonist valsartan . It reduces platelet aggregation induced by epinephrine and collagen but not ADP in human whole blood.
T16477	PF-03715455	p38 MAPK	MAPK
	PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 is an effective inhibitor of inhaled p38 MAPK. PF-03715455 displays some selectivity for p38α over p38β (respective IC50: 0.88 and 23 nM). PF-0371545
T63575	PF-8380 hydrochloride
	PF-8380 hydrochloride 是一种有效的autotaxin 抑制剂，体外酶实验和人类全血细胞实验中，IC50分别为 2.8 nM 和 101 nM。
T37842	ASB 14780
	Potent and selective cytosolic phospholipase A2 alpha (cPLA2α) inhibitor (IC50 = 20 nM). Selective for cPLA2α over secreted PLA2α (sPLA2α; exhibits no inhibition at 10 μM). Inhibits cPLA2α-dependent inflammatory responses in vitro in guinea pig and human whole-blood assays. Improves diet-induced liver injury and CCl4-induced hepatic fibrosis in vivo. Orally bioavailable.
T35947	17(S)-HDHA
	17(S)-HDHA is a primary mono-oxygenation product of docosahexaenoic acid in human whole blood, human leukocytes, and mouse brain. 17(S)-HDHA serves as a precursor to 17(S)-resolvins and has intrinsic biological activity, such as the inhibition of TNF-α-induced interleukin-1β expression in human glioma cells and inhibition of TNF-α-induced leukocyte trafficking to the mouse air pouch.
T40123	BMS-986251
	BMS-986251 is a potent and specific RORγt inverse agonist that exerts its action via oral administration. It shows an EC 50 of 12 nM for RORγt GAL4. In human whole blood assay, BMS-986251 effectively inhibits IL-17 with an EC 50 of 24 nM. Furthermore, BMS-986251 exhibits strong therapeutic effects in mouse acanthosis and Imiquimod-induced models, which are commonly used preclinical models for psoriasis.
T28405	Phe-Pro-Arg-PABA-Resorufin
	Phe-Pro-Arg-PABA-Resorufin is a Chromogenic and fluorogenic peptide substrate for the highly sensitive detection of proteases in biological matrices. The substrate is also applicable to the sensitive detection of the thrombin inhibitor dabigatran in human
T36923	CXCR2-IN-2 CXCR2-IN-2
	CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM[1]. CXCR2-IN-2 (compound 68) (1-10 mg/kg; p.o.; twice daily for 3 days) dose-dependently reduces neutrophil infiltration in vivo in ra...
T71510	MF-592
	MF-592 is a potent and selective antagonists of the EP4 receptor. MF-592 demonstrated good functional potency (hEP4 IC50 = 3 nM) and potent inhibition of PGE2 modulated TNFa release in LPS stimulated human whole blood (hWB) (IC50 = 78nM). In addition, it showed an excellent oral pharmacokinetic (PK) profile and in vivo efficacy in a rat chronic adjuvant-induced-arthritis model (ED50 = 0.1 mg/kg/day).. MF-592 has a desirable overall preclinical profile that suggests it is suitable for further de...
T71300	Pentoxifylline-d6
	Pentoxifylline-d6 is intended for use as an internal standard for the quantification of pentoxifylline by GC- or LC-MS. Pentoxifylline is a hemorrheologic agent. It increases the deformability of washed isolated human erythrocytes when used at a concentration of 100 µM. Pentoxifylline (1, 2, and 3 mM) inhibits ADP-induced platelet aggregation in isolated human whole blood. It inhibits thrombus formation induced by ADP in a hamster cheek pouch model when administered at doses of 5, 10, and 20 mg/...
T78175	JAK-IN-25	JAK	Angiogenesis; Chromatin/Epigenetic; JAK/STAT signaling; Stem Cells
	JAK-IN-25（化合物19）是一种高效的JAK抑制剂，对TYK2、JAK1、JAK2和JAK3的IC50值分别为6 nM、21 nM、8 nM、1051 nM。该化合物还能抑制人全血中IL-12（HEB IL-12），IC50为28 nM，显示其在癌症研究中的潜在应用价值。
T62451	TYK2-IN-12
	TYK2-IN-12 (compound 30) 是一种选择性的、口服具有活力的 TYK2 (酪氨酸激酶 2) 抑制剂 (Ki: 0.51 nM)。TYK2-IN-12 对 IL-12 诱导的人和小鼠全血中 IFNγ 具有抑制作用，他们的 IC50 值分别为 2.7 和 7.0 μM。TYK2-IN-12 能够用于研究银屑病。
T35864	T-5342126
	T-5342126 is a toll-like receptor 4 (TLR4) antagonist.1It reduces LPS-induced production of nitric oxide (NO) in RAW 264.7 cells (IC50= 27.8 μM), as well as decreases LPS-induced IL-8, TNF-α, and IL-6 production in isolated human whole blood (IC50s = 110.5, 315.6, and 318.4 μM, respectively). T-5342126 (82 mg/kg) reduces ethanol intake and the abundance of ionized calcium-binding adapter molecule 1 (Iba1), a marker of microglial activation, in the central nucleus of the amygdala in ethanol-depen...
T68321	AS1940477
	AS1940477 is p38 MAPK inhibitor. AS1940477 inhibited the enzymatic activity of recombinant p38α and β isoforms but showed no effect against other 100 protein kinases including p38γ and δ isoforms. In human peripheral blood mononuclear cells, AS1940477 inhibited lipopolysaccharide (LPS)- or phytohemagglutinin A (PHA)-induced production of proinflammatory cytokines, including TNFα, IL-1β, and IL-6 at low concentrations (LPS/TNFα, IC(50)=0.45n M; PHA/TNFα, IC(50)=0.40 nM). In addition, equivalent c...
T36167	8-iso-15-keto Prostaglandin F2β 8-iso-15-keto Prostaglandin F2β
	8-iso Prostaglandin F2β (8-iso PGF2β) is an isomer of PGF2α of non-enzymatic origin. It is one of 64 possible isomers of PGF2α which can be produced by free radical peroxidation of arachidonic acid. 8-iso PGF2β exhibits very weak contraction of human umbilical vein artery and does not promote aggregation of human whole blood. However, 8-iso PGF2β moderately contracts both the canine and porcine pulmonary vein, although the effect is much weaker than that exhibited by other isoprostanes such as 8...
T35536	Tpl2 Kinase Inhibitor (hydrochloride)
	Tpl2 kinase inhibitor is an inhibitor of tumor progression locus 2 (Tpl2; IC50= 0.05 μM).1It is selective for Tpl2 over MEK, p38 MAPK, Src, MK2, and PKC (IC50s = >40, 180, >400, 110, and >400 μM, respectively). Tpl2 kinase inhibitor inhibits LPS-induced TNF-α production in isolated human monocytes and whole blood (IC50s = 0.7 and 8.5 μM, respectively). It enhances differentiation induced by calcitriol in HL-60 and U937 leukemia cells when used at a concentration of 5 μM.2Tpl2 kinase inhibitor (5...
T12793	(S)-BI 665915	Others	Others
	(S)-BI 665915 is an orally active inhibitor of oxadiazole-containing 5-lipoxygenase-activating protein (FLAP)(IC50 of 1.7 nM for FLAP binding)..

化合物

Cat.No: T9020

Target: Epigenetic Reader Domain

Cat.No: T14975

Synonym: CJ-042794

Target: Others

Cat.No: T32824

Synonym: LM 1685,LM1685

Target: COX

Cot inhibitor-2

Cat.No: T10866

Target: TNF, MAPK

Cat.No: T26531

Synonym: ABT963

Cot inhibitor-1 hydrochloride

Cat.No: T10865L

Synonym: Cot inhibitor-1 hydrochloride(915365-57-0 Free base)

Target: TNF, MAPK

Cat.No: T68155

Target: Prostaglandin Receptor, LTR

Cat.No: T3631

Target: PDE

Cot inhibitor-1

Cat.No: T10865

Target: TNF, MAPK

Cat.No: T0463

Synonym: Loxoprofene,洛索洛芬,Loxoprofeno,Koloxo

Target: COX

Cat.No: T14374

Cat.No: T14381

Synonym: AZD-7624

Target: p38 MAPK, TNF

4-hydroxy Valsartan

Cat.No: T35725

Cat.No: T16477

Target: p38 MAPK

PF-8380 hydrochloride

Cat.No: T63575

Cat.No: T37842

Cat.No: T35947

Cat.No: T40123

Phe-Pro-Arg-PABA-Resorufin

Cat.No: T28405

Cat.No: T36923

Synonym: CXCR2-IN-2

Cat.No: T71510

Pentoxifylline-d6

Cat.No: T71300

Cat.No: T78175

Target: JAK

Cat.No: T62451

Cat.No: T35864

Cat.No: T68321

8-iso-15-keto Prostaglandin F2β

Cat.No: T36167

Synonym: 8-iso-15-keto Prostaglandin F2β

Tpl2 Kinase Inhibitor (hydrochloride)

Cat.No: T35536

Cat.No: T12793

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T7786	Tryptanthrin	DNA gyrase	DNA Damage/DNA Repair
	Tryptanthrin 是一种口服具有活性的细胞内Leukotriene (LT) biosynthesis 抑制剂。它能够降低大鼠胸膜炎模型中的 LTB4 水平，并抑制人全血中Leukotriene 的形成 (IC50= 10 µM)。
TN5661	1,7-Bis(4-hydroxyphenyl)-3-hydroxy-1,3-heptadien-5-one
	1,7-Bis(4-hydroxyphenyl)-3-hydroxy-1,3-heptadien-5-one shows strong inhibition of collagen-induced, arachidonic acid-induced, and adenosine diphosphate-induced platelet aggregation of human whole blood.
T40193	Ebeiedinone
	Ebeiedinone, a steroidal alkaloid derived from Fritillaria species, effectively inhibits the activity of human whole blood cholinesterase (ChE) at a concentration of 0.1 mM, resulting in a significant inhibitory effect of 69.0%.

天然产物

Cat.No: T7786

Target: DNA gyrase

1,7-Bis(4-hydroxyphenyl)-3-hydroxy-1,3-heptadien-5-one

Cat.No: TN5661

Cat.No: T40193

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