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28

抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T36531	PAR2 (1-6) (mouse, rat) PAR2 (1-6) (mouse, rat)
	PAR2 (1-6) is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of mouse and rat PAR2. It also corresponds to residues 39-44 and 37-42 of the mouse and rat full-length sequences, respectively. PAR2 (1-6) induces relaxation in precontracted rat arteries in a concentration-dependent manner, an effect that can be reduced by the nitric oxide synthase inhibitor L-NNA . It inhibits keratinocyte growth i...
T35955	PAR2 (1-6) amide (human) (trifluoroacetate salt) PAR2 (1-6) amide (human) (trifluoroacetate salt)
	PAR2 (1-6) amide is a synthetic peptide agonist of proteinase-activated receptor 2 (PAR2) that corresponds to residues 1-6 of the amino terminal tethered ligand sequence of human PAR2 and residues 37-42 of the full-length sequence.1It binds to NCTC 2544 cells expressing human PAR2 (Ki= 9.64 μM in a radioligand binding assay) and induces calcium mobilization in the same cells (EC50= 0.075 μM).2PAR2 (1-6) amide (100 μM) reduces colony formation of A549 lung cancer cells.1It induces superoxide prod...
T8917	PAR-2-IN-1 IUN76750,8-(叔丁基)-6-氯咪唑并[1,2-B]吡啶-2-羧酸甲酯	Protease-activated Receptor	GPCR/G Protein
	PAR-2-IN-1 (IUN76750) 是一种 PAR-2 信号通路抑制剂，具有抗炎和抗癌作用。
TP1046L	PAR-2 Activating Peptide acetate SLIGRL-NH2 acetate,PAR-2 Activating Peptide acetate(171436-38-7 free base),Protease-Activated Receptor-2 Activating Peptide acetate	Protease-activated Receptor	GPCR/G Protein
	PAR-2 Activating Peptide acetate (SLIGRL-NH2 acetate)(171436-38-7 free base) 是 Protease-Activated Receptor-2 (PAR-2) 的激动剂。
T7513	Protease-Activated Receptor-2, amide 蛋白酶活化的受体-2，酰胺,SLIGKV-NH2,H-丝氨酰亮氨酰异亮氨酰甘氨酰赖氨酰缬氨酰NH2	Protease-activated Receptor	GPCR/G Protein
	Protease-Activated Receptor-2, amide (SLIGKV-NH2) 是 PAR2 的激动剂，IC50为 10.4 M。
TQ0012	AZ3451	Protease-activated Receptor	GPCR/G Protein
	AZ3451 是蛋白酶激活受体 2 的变构拮抗剂，IC50值为 23 nM。
T2370	AC-55541 AOB2796	Proteasome; Protease-activated Receptor	GPCR/G Protein; Proteases/Proteasome; Ubiquitination
	AC-55541 (AOB2796) 是高选择性的蛋白酶激活受体 2(PAR2)激动剂，pEC50为6.7。它在 PI 水解测定和 Ca2+动态测定中的pEC50值为 5.9 和 6.6，在体内表现出伤害感受器活性。
T21699L	VKGILS-NH2 Acetate VKGILS-NH2 Acetate (942413-05-0 Free base)	Protease-activated Receptor	GPCR/G Protein
	VKGILS-NH2 Acetate 是 SLIGKV-NH2 的反向氨基酸序列控制肽，SLIGKV-NH2 是一种蛋白酶激活受体 2 (PAR2) 激动剂。
TP1378	2-Furoyl-LIGRLO-amide TFA(729589-58-6 free base) 2-Furoyl-LIGRLO-amide	Protease-activated Receptor	GPCR/G Protein
	2-Furoyl-LIGRLO-amide TFA(729589-58-6 free base) 是一种有效的选择性蛋白酶激活受体 2 (PAR2) 激动剂。
T7137	I-191	Protease-activated Receptor	GPCR/G Protein
	I-191 是选择性有效的蛋白酶激活受体 2 拮抗剂。
TP1904L	FSLLRY-NH2 TFA(245329-02-6 free base)	Protease-activated Receptor	GPCR/G Protein
	FSLLRY-NH2 TFA(245329-02-6 free base) 是一种蛋白酶激活受体 2 (PAR2) 抑制剂。在 ICR 小鼠中逆转紫杉醇诱导的机械异常性疼痛、热痛觉过敏和 PKC 激活。阻断分离的心脏成纤维细胞中的 ERK 活化和胶原蛋白生成。还可以减轻皮肤癣菌相关瘙痒小鼠模型的症状。
T41190	AY 77 Unk-Cha-Chg-NH2	ERK; Calcium Channel; Protease-activated Receptor	GPCR/G Protein; MAPK; Membrane transporter/Ion channel; Metabolism
	AY 77 (Unk-Cha-Chg-NH2)是一种有效的、具有选择性的 PAR2激动剂。AY 77对 Ca2+和 ERK1/2信号显示出选择性(Ca2+释放的ec50值为40 nM, ERK1/2磷酸化的ec50值为2 μM)。AY 77能够促进人乳腺癌细胞的体外迁移。
T11369L	GB-110 hydrochloride (1252806-70-4 free base) GB-110 hydrochloride	Others	Others
	GB-110 hydrochloride selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM. GB-110 hydrochloride is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist.
T11370	GB-88	Others	Others
	GB-88 is an selective , oral non-peptide antagonist of PAR2, inhibits PAR2 activated Ca2+ release with an IC50 of 2 μM.
T75871	FSLLRY-NH2 TFA
	FSLLRY-NH2 TFA 是蛋白酶激活受体2(PAR2)抑制剂。
TP1478	2-Furoyl-LIGRLO-amide 2-Furoyl-LIGRLO-amide TFA(729589-58-6,FREE)
	2-Furoyl-LIGRLO-amide TFA is a peptide that acts as a proteinase-activated receptor-2 (PAR2) agonist, and contains a furoyl group addition at its N-terminal.
T27406	GB83 GB-83,GB 83
	GB83 is a selective human protease activated receptor 2 (PAR2) antagonist.
T11369	GB-110	Others	Others
	GB-110 selectively induces PAR2-mediated intracellular Ca2+ release in HT29 cells with an EC50 of 0.28 μM. GB-110 is a potent, orally active, and nonpeptidic protease activated receptor 2 (PAR2) agonist.
T4186	AC-264613 AC264613	Protease-activated Receptor	GPCR/G Protein
	AC-264613 是一种选择性蛋白酶激活受体 (PAR-2) 激动剂，pEC50为 7.5。
T73854	GB-110 hydrochloride
	GB-110 hydrochloride 是一种有效的，具有口服活性的，非肽类的 protease activated receptor2 (PAR2)激动剂。GB-110 hydrochloride 选择性诱导 PAR2介导的 HT29 细胞内 Ca2+释放，EC50值为 0.28 μM。
T75905	2-Furoyl-LIGRLO-amide TFA
	2-Furoyl-LIGRLO-amide TFA 为高效选择性PAR2 (蛋白酶激活受体2) 激动剂，pD2值达7.0。
T60319	AZ8838
	AZ8838 是一种有效的、竞争性的、变构的、口服活性的 PAR2非肽小分子拮抗剂，其对 hPAR2 的 pKi 值为 6.4。
T75903	VKGILS-NH2 TFA
	VKGILS-NH2 TFA 是SLIGKV-NH2（PAR2激动剂）的逆序反向对照肽，无影响细胞DNA合成。
T22933	LRGILS-NH2	Others	Others
	LRGILS-NH2 is a reversed amino acid sequence control peptide for SLIGRL-NH2, a protease-activated receptor-2 (PAR2) agonist that facilitates gastrointestinal transit in vivo.
TP1904	FSLLRY-NH2
	Selective PAR2 peptide antagonist. Reverses taxol-induced mechanical allodynia, heat hyperalgesia and PKC activation in ICR mice. Blocks ERK activation and collagen production in isolated cardiac fibroblasts. Also reduces symptoms in a mouse model of derm
T41189	AY 254
	AY 254 is a potent PAR2 biased agonist. Selectively activates ERK1/2 signaling (EC50= 2 nM for ERK1/2 phosphorylation versus 80 nM for Ca2+release). Reduces cytoKi ne-induced caspase 3/8 activation, promotes scratch-wound healing, and induces IL-8 secretion, in human colorectal cancer (HT29) cellsin vitro.
T78672	I-287
	I-287为一种口服活性PAR2选择性抑制剂，能对Gαq和Gα12/13的活性以及其下游效应物施加负异构调控。该化合物能够减轻Complete Freund's adjuvant引发的小鼠炎症，适用于免疫炎症研究。
T60854	ENMD-1068 hydrochloride
	ENMD-1068 hydrochloride 是一种选择性的蛋白酶激活受体 2 (PAR2) 拮抗剂。ENMD-1068 hydrochloride 可通过抑制TGF-β1/Smad 信号转导而减少肝星状细胞的活化和胶原蛋白的表达。ENMD-1068 hydrochloride 还能抑制子宫内膜细胞的增殖，并诱导病灶中上皮细胞的凋亡。ENMD-1068 hydrochloride 可用于子宫内膜异位症、肝纤维化的研究。

化合物

PAR2 (1-6) (mouse, rat)

Cat.No: T36531

Synonym: PAR2 (1-6) (mouse, rat)

PAR2 (1-6) amide (human) (trifluoroacetate salt)

Cat.No: T35955

Synonym: PAR2 (1-6) amide (human) (trifluoroacetate salt)

Cat.No: T8917

Synonym: IUN76750,8-(叔丁基)-6-氯咪唑并[1,2-B]吡啶-2-羧酸甲酯

Target: Protease-activated Receptor

PAR-2 Activating Peptide acetate

Cat.No: TP1046L

Synonym: SLIGRL-NH2 acetate,PAR-2 Activating Peptide acetate(171436-38-7 free base),Protease-Activated Receptor-2 Activating Peptide acetate

Target: Protease-activated Receptor

Protease-Activated Receptor-2, amide

Cat.No: T7513

Synonym: 蛋白酶活化的受体-2，酰胺,SLIGKV-NH2,H-丝氨酰亮氨酰异亮氨酰甘氨酰赖氨酰缬氨酰NH2

Target: Protease-activated Receptor

Cat.No: TQ0012

Target: Protease-activated Receptor

Cat.No: T2370

Synonym: AOB2796

Target: Proteasome, Protease-activated Receptor

VKGILS-NH2 Acetate

Cat.No: T21699L

Synonym: VKGILS-NH2 Acetate (942413-05-0 Free base)

Target: Protease-activated Receptor

2-Furoyl-LIGRLO-amide TFA(729589-58-6 free base)

Cat.No: TP1378

Synonym: 2-Furoyl-LIGRLO-amide

Target: Protease-activated Receptor

Cat.No: T7137

Target: Protease-activated Receptor

FSLLRY-NH2 TFA(245329-02-6 free base)

Cat.No: TP1904L

Target: Protease-activated Receptor

Cat.No: T41190

Synonym: Unk-Cha-Chg-NH2

Target: ERK, Calcium Channel, Protease-activated Receptor

GB-110 hydrochloride (1252806-70-4 free base)

Cat.No: T11369L

Synonym: GB-110 hydrochloride

Target: Others

Cat.No: T11370

Target: Others

Cat.No: T75871

2-Furoyl-LIGRLO-amide

Cat.No: TP1478

Synonym: 2-Furoyl-LIGRLO-amide TFA(729589-58-6,FREE)

Cat.No: T27406

Synonym: GB-83,GB 83

Cat.No: T11369

Target: Others

Cat.No: T4186

Synonym: AC264613

Target: Protease-activated Receptor

GB-110 hydrochloride

Cat.No: T73854

2-Furoyl-LIGRLO-amide TFA

Cat.No: T75905

Cat.No: T60319

Cat.No: T75903

Cat.No: T22933

Target: Others

Cat.No: TP1904

Cat.No: T41189

Cat.No: T78672

ENMD-1068 hydrochloride

Cat.No: T60854

Cat. No.	Product Name	Target	Signaling Pathways
TN6872	Trypsin	Protease-activated Receptor	GPCR/G Protein
	Trypsin 是一种可从鱼类分离出的丝氨酸蛋白酶，可水解赖氨酸或精氨酸羧基侧蛋白质。Trypsin 具有抗炎活性，可通过 PDCoV 的 S 糖蛋白与 pAPN 的相互作用诱导 PDCoV 感染的细胞膜融合，可激活 PAR2 和 PAR4，促进细胞增殖和分化。Trypsin 可用于促进伤口愈合和研究神经源性炎症。

天然产物

Cat.No: TN6872

Target: Protease-activated Receptor

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