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30

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T13292	VDR agonist 1	Others	Others
	VDR agonist 1 (compound 28) 是一种非甾体类维生素 D 受体 (VDR)的激动剂，在MCF-7 细胞中测得其IC50值为 690 nM。VDR agonist 1 通过上调 p21 和 p27 的表达来抑制细胞周期，通过增加 BAX 的表达来促进细胞凋亡，降低 Bcl-2 的表达，具有治疗乳腺癌的潜力。
T78944	VDR agonist 2
	VDR agonist 2（化合物16i）作为VDR（vitamin D receptor）激动剂，能有效抑制TGF-β1诱导的肝星状细胞（HSC）活化，并在体外和体内展现出显著的抗肝纤维化效果。
TQ0200	Paricalcitol
	Paricalcitol 是一种 vitamin D receptor 激活剂，是一种 vitamin D 类似物，用于研究继发性甲状旁腺功能亢进，该疾病与慢性肾功能衰竭有关。
T24166	Inecalcitol TX 522,TX-522,TX522,伊奈骨化醇	Apoptosis	Apoptosis
	Inecalcitol (TX 522) 是一种独特的维生素 D3 类似物，可诱导细胞凋亡，有抗癌活性。它是一种具有口服活性维生素 D 受体激动剂，Kd 为 0.53 nM。
T16015	Maxacalcitol 马沙骨化醇,22-Oxacalcitriol	Others	Others
	Maxacalcitol (22-Oxacalcitriol) 是非血钙维生素 D3的一种类似物，是 VDR 样受体的配体。
T14856	Calcipotriol MC 903,卡泊三醇,Calcipotriene
	Calcipotriol (MC 903) 是一种合成的 VitD3类似物，对维他命 D 受体具有高亲和力。
TQ0244	Calcipotriol monohydrate 钙泊三醇一水合物,卡泊三醇一水合物
	Calcipotriol monohydrate 是维生素 D3 的类似物，对维生素 D 受体具有高亲和力。Calcipotriol monohydrate 可用于银屑病研究。
T6430L	Calcifediol monohydrate 骨化二醇一水合物,25-hydroxy Vitamin D3 monohydrate	Endogenous Metabolite	Metabolism
	Calcifediol monohydrate (25-hydroxy Vitamin D3 monohydrate) 是维生素 D3 在肝中经羟基化后得到的前激素，是有效的 VDR 抑制剂。
T6112	Doxercalciferol TSA 840,度骨化醇,Hectorol,1.alpha.-Hydroxyvitamin D2,1α-hydroxyvitamin D2	Others	Others
	Doxercalciferol (TSA 840) 是一种维生素 D2 类似物，是一种维生素 D 受体激活剂，能够阻碍肾病的进程。
T6374	Alfacalcidol Bondiol,Etalpha,阿法骨化醇,1-hydroxy Vitamin D3,1.alpha.-Hydroxyvitamin D3,1-hydroxycholecalciferol	Others	Others
	Alfacalcidol (Etalpha) 是一种维生素 D3 衍生物，是非选择性的维生素 D 受体活化剂，有用于骨质疏松研究的潜力。
T13404	ZK168281	Others	Others
	ZK168281 is a 25-carboxylic ester 1α,25(OH)2D3 analog and a pure antagonist of VDR (Kd of 0.1 nM). ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor.
T24675	PS121912 PS-121912,PS 121912
	PS121912 is a potent and selective inhibitor of VDR-coactivator.
T69676	LG190155
	LG190155 is a moderately potent VDR agonist. Vitamin D receptor (VDR) agonists are well known for their capacity to control calcium and bone metabolism and to regulate growth and differentiation of many cell types.
T70151	MeTC7
	MeTC7 is a VDR antagonist, which can be synthesized from 7-dehydrocholesterol (6) in two steps, inhibits VDR selectively, suppresses the viability of cancer cell-lines, and reduces the growth of the spontaneous transgenic TH-MYCN neuroblastoma and xenografts in vivo.
T11952	Maxacalcitol-D6	Others	Others
	Maxacalcitol-D6 is a non-calcemic vitamin D3 analog and VDR ligand of VDR-like receptors.Maxacalcitol-D6 is the deuterated form of Maxacalcitol (22-Oxacalcitriol).
T75123	Maxacalcitol-d
	Maxacalcitol-d66是Maxacalcitol (22-Oxacalcitriol)的氘化形式，是非血钙维生素D3类似物和VDR 样受体VDR 配体。
T17292	ZK159222	Others	Others
	ZK159222 is an effective 1α,25-(OH)2D3 receptor (VDR) agonist. ZK159222 has a partial agonistic character.
T27825	LG190178 LG-190178,LG 190178
	LG190178, a vitamin D receptor (VDR) ligand, is a therapeutic agent used for the treatment of psoriasis, osteoporosis, and secondary hyperparathyroidism.
T36593	TEI-9648
	TEI-9648, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9648 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9648 also inhibits HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9648 has the potential for bone metabolism research[1][2]. TEI-9648 (10-1000 nM) dose-dependently blocks the reciprocal changes of CD11b and CD71 expression associated with HL-60 cell differentiation induced by 1α,25(OH)2D3[1]. TEI-9648 has cons...
T13590	Calcipotriol Impurity C	Others	Others
	Calcipotriol Impurity C is the impurity of Calcipotriol. Calcipotriol is a VDR-like receptors ligand.
TQ0123	MC 1046 Impurity A of Calcipotriol	Others	Others
	MC 1046 is an impurity of Calcipotriol. Calcipotriol is a ligand of VDR-like receptors.
T11644	Impurity C of Alfacalcidol	Others	Others
	Impurity of Alfacalcidol is an impurity of Alfacalcidol. Alfacalcidol is a non-selective VDR activator medication.
T17031	TEI-9647	Others	Others
	TEI-9647 is a 1α,25-dihydroxy vitamin D3-26,23-lactone (1α,25-lactone) analog and is an effective VDR/vitamin D-responsive element (DRE)-mediated genomic actions antagonist.
T10279	Alfacalcidol-D6	Others	Others
	Alfacalcidol-D6 is a deuterated Alfacalcidol. Alfacalcidol is a non-selective VDR activator medication.
T10088	24R-Calcipotriol PRI 2202	Others	Others
	24R-Calcipotriol(PRI 2202) is an impurity of Calcipotriol which is a ligand of VDR-like receptors.
T11646	Impurity F of Calcipotriol	Others	Others
	Impurity F of Calcipotriol is a impurity of Calcipotriol. Calcipotriol (MC 903; Calcipotriene) is a ligand of VDR-like receptors.
T9644	Triciferol
	Triciferol 作为具有结合了 VDR 激动剂和 HDAC 拮抗剂活性的多重配体发挥作用。Triciferol 直接与 VDR 结合 (IC50=87 nM)，在一些 1,25D 靶基因上作为具有 1,25D 样效力的激动剂发挥作用。Triciferol 诱导显著的微管蛋白高乙酰化，并增强组蛋白乙酰化。Triciferol 在体外癌细胞模型中也表现出有效的抗增殖和细胞毒性活性。
T35524	(1S)-Calcitriol
	(1S)-Calcitriol (1α,25-Dihydroxy-3-epi-vitamin-D3) is a natural metabolite of 1α,25-dihydroxyvitamin D3 (1α,25(OH)2D3). (1S)-Calcitriol exhibits potent vitamin D receptor (VDR)-mediated actions such as inhibition of keratinocyte growth or suppression of parathyroid hormone secretion[1]. 3‐epi‐Calcitroic acid is an end product of (1S)-Calcitriol (1α,25-Dihydroxy-3-epi-vitamin-D3; 3‐epi‐1a,25(OH)2D3) metabolism by rat CYP24A1[1]. [1]. Steve Y Rhieu, et al. Metabolic stability of 3-epi-1α,25-dihydr...
T11643	Impurity B of Calcitriol 1β,25-Dihydroxyvitamin-D3,1-Epicalcitriol	Others	Others
	Impurity B of Calcitriol is an impurity of Calcitriol. Calcitriol is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
T83765	Dendrogenin A DDA
	Dendrogenin A (DDA) 作为一种选择性肝X受体(LXR)调节剂(SLiM)、胆固醇环氧水解酶(ChEH; Ki = 120 nM)的抑制剂及胆固醇的活性代谢产物，通过DDA合成酶将5,6α-环氧胆固醇与组胺结合形成。DDA在非癌性人乳腺上皮细胞和上皮黑色素细胞中存在，但在多种乳腺癌细胞或黑色素瘤细胞中未发现，且在分离的人乳腺肿瘤组织中仅以低水平存在。它抑制22(R)-羟基胆固醇诱导的LXRβ和LXRα激活(分别以IC50 = 76和362 nM)，但也是LXR的部分激动剂，在B16/F10小鼠黑色素瘤细胞中增加Nur77、NOR-1、LC3-I和LC3-II的蛋白水平。DDA选择性调节LXRα和LXRβ，而非孕烯X受体(PXR)、芳香烃受体(AhR)、维生素D受体(VDR)、维甲酸X受体γ(RXRγ)、维甲酸受体α(RARα)、过氧化物酶体增殖物激活受体α(PPARα)、PPARγ、糖皮质激素受体、雄激素受体、雌激素受体α(ERα)及ERβ在2.5 µM下。此外，DDA在2.5和5 µM的浓度下增加B16/F10和SK-MEL-28癌细胞中LC3-II的蛋白水平，并在2...

化合物

VDR agonist 1

Cat.No: T13292

Target: Others

VDR agonist 2

Cat.No: T78944

Cat.No: TQ0200

Cat.No: T24166

Synonym: TX 522,TX-522,TX522,伊奈骨化醇

Target: Apoptosis

Cat.No: T16015

Synonym: 马沙骨化醇,22-Oxacalcitriol

Target: Others

Cat.No: T14856

Synonym: MC 903,卡泊三醇,Calcipotriene

Calcipotriol monohydrate

Cat.No: TQ0244

Synonym: 钙泊三醇一水合物,卡泊三醇一水合物

Calcifediol monohydrate

Cat.No: T6430L

Synonym: 骨化二醇一水合物,25-hydroxy Vitamin D3 monohydrate

Target: Endogenous Metabolite

Doxercalciferol

Cat.No: T6112

Synonym: TSA 840,度骨化醇,Hectorol,1.alpha.-Hydroxyvitamin D2,1α-hydroxyvitamin D2

Target: Others

Cat.No: T6374

Synonym: Bondiol,Etalpha,阿法骨化醇,1-hydroxy Vitamin D3,1.alpha.-Hydroxyvitamin D3,1-hydroxycholecalciferol

Target: Others

Cat.No: T13404

Target: Others

Cat.No: T24675

Synonym: PS-121912,PS 121912

Cat.No: T69676

Cat.No: T70151

Maxacalcitol-D6

Cat.No: T11952

Target: Others

Cat.No: T75123

Cat.No: T17292

Target: Others

Cat.No: T27825

Synonym: LG-190178,LG 190178

Cat.No: T36593

Calcipotriol Impurity C

Cat.No: T13590

Target: Others

Cat.No: TQ0123

Synonym: Impurity A of Calcipotriol

Target: Others

Impurity C of Alfacalcidol

Cat.No: T11644

Target: Others

Cat.No: T17031

Target: Others

Alfacalcidol-D6

Cat.No: T10279

Target: Others

24R-Calcipotriol

Cat.No: T10088

Synonym: PRI 2202

Target: Others

Impurity F of Calcipotriol

Cat.No: T11646

Target: Others

Cat.No: T9644

(1S)-Calcitriol

Cat.No: T35524

Impurity B of Calcitriol

Cat.No: T11643

Synonym: 1β,25-Dihydroxyvitamin-D3,1-Epicalcitriol

Target: Others

Cat.No: T83765

Synonym: DDA

Cat. No.	Product Name	Target	Signaling Pathways
T1086	Vitamin D2 Calciferol,Ergocalciferol,Ercalciol,维生素D2	DNA/RNA Synthesis; Endogenous Metabolite	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Metabolism
	Vitamin D2 (Calciferol) 来源于植物或膳食补充剂，能够用作维生素 D 的补充剂。
T1135	Vitamin D3 维生素D3,Cholecalciferol,Colecalciferol	Endogenous Metabolite	Metabolism
	Vitamin D3 (Cholecalciferol) 是维生素 D 的一种天然存在形式，代谢激活后可以诱导细胞分化和癌细胞增殖。
T6316	Calcitriol Topitriol,Rocaltrol,Calcijex,RO215535,骨化三醇,1,25-Dihydroxyvitamin D3	Endogenous Metabolite	Metabolism
	Calcitriol (1,25-Dihydroxyvitamin D3) 是一种维他命 D 的代谢物，一种维他命 D 受体 (VDR) 的激动剂 (IC50=0.4 nM)。Calcitriol 增加肠道对钙和磷的吸收，并与甲状旁腺激素一起增加了骨吸收。
T6430	Calcifediol 25-羟基维生素 D3,U 32070E,25-hydroxy Vitamin D3,RO 8-8892,骨化二醇	Endogenous Metabolite	Metabolism
	Calcifediol (U 32070E) 是由维生素 D3 在肝中经羟基化后得到的前激素，是 VDR 的有效抑制剂。

天然产物

Cat.No: T1086

Synonym: Calciferol,Ergocalciferol,Ercalciol,维生素D2

Target: DNA/RNA Synthesis, Endogenous Metabolite

Cat.No: T1135

Synonym: 维生素D3,Cholecalciferol,Colecalciferol

Target: Endogenous Metabolite

Cat.No: T6316

Synonym: Topitriol,Rocaltrol,Calcijex,RO215535,骨化三醇,1,25-Dihydroxyvitamin D3

Target: Endogenous Metabolite

Cat.No: T6430

Synonym: 25-羟基维生素 D3,U 32070E,25-hydroxy Vitamin D3,RO 8-8892,骨化二醇

Target: Endogenous Metabolite

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