SPA70

CAT: 0804-HY-124830-01Size: 1 mgDry Ice: NoHazardous: No

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CAT#:0804-HY-124830-01Size:1 mg

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Description

SPA70 is an orally available, selective, competitive antagonist of the human pregnane X receptor (hPXR) (IC50=540 nM), which blocks the hPXR nuclear receptor signaling pathway and its mediated transcriptional activation of drug metabolizing enzymes (e.g., CYP3A4, MDR1) . SPA70 exhibits low toxicity in both in vitro and in vivo models and can be used to study hPXR-mediated cancer drug resistance and liver injury[1][2][3].

CAS Number

931314-31-7

UNSPSC

12352005

Target

Pregnane X Receptor (PXR)

Type

Reference compound

Related Pathways

Vitamin D Related/Nuclear Receptor

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/spa70.html

Purity

99.0

Solubility

DMSO : 40 mg/mL (ultrasonic; warming)

Smiles

CC1=C(S(=O)(C2=CC=C(C(C)(C)C)C=C2)=O)N=NN1C3=CC(OC)=CC=C3OC

Molecular Formula

C21H25N3O4S

Molecular Weight

415.51

References & Citations

[1]Lin W, et, al. SPA70 is a potent antagonist of human pregnane X receptor. Nat Commun. 2017 Sep 29;8 (1) :741.|[2]Niu X, et al. Combination of Paclitaxel and PXR Antagonist SPA70 Reverses Paclitaxel-Resistant Non-Small Cell Lung Cancer. Cells. 2022 Oct 1;11 (19) :3094.|[3]Xie Y, et al. Activation of Pregnane X Receptor Sensitizes Mice to Hemorrhagic Shock-Induced Liver Injury. Hepatology. 2019 Sep;70 (3) :995-1010.

Shipping Conditions

Blue Ice

Storage Conditions

-20°C, 3 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

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