BiochemProbe — Life Science Research Reagents

LRH-1 modulator-1 free base

LRH-1 agonist-2 is a selective, full LRH-1 agonist.

For research use only. Not for human or veterinary use.

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LRH-1 modulator-1 structure

CAS No.: 2244781-29-9

Download structure (.mol)

Pack sizes & pricing

Size Price SKU Stock
5 mg USD 680.00 BP-02170-5mg In stock Get quote
10 mg USD 1,150.00 BP-02170-10mg In stock Get quote
25 mg USD 2,280.00 BP-02170-25mg In stock Get quote
50 mg USD 3,600.00 BP-02170-50mg In stock Get quote

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Description

LRH-1 agonist-2 (Compound 6N) is a selective, full LRH-1 agonist with an EC50 of 15.7 nM. LRH-1 agonist-2 directly interacts with the Thr352 and His390 residues in the LRH-1 binding pocket, promotes allosteric signaling to the activation function surface (AFS), stabilizes the AFS and enhances coactivator recruitment. LRH-1 agonist-2 induces the anti-inflammatory cytokine IL-10, and reduces the pro-inflammatory cytokines IL-1β and TNFα. LRH-1 modulator-1 exerts anti-inflammatory effects in intestinal organoids. LRH-1 modulator-1 can be used in studies related to inflammatory bowel disease.

Biological activity

In Vitro LRH-1 modulator-1 potently activates the transcriptional activity of LRH-1 in Hela cells with an EC50 of 15.7 nM, and this activity depends on the interaction with LRH-1 residues Thr352 and His390.

Identifiers

SMILES
CCCCCCC1=C([C@@]2(CC[C@@H]([C@@H]2C1)NS(=O)(=O)N)C(=C)C3=CC=CC=C3)C4=CC=CC=C4
InChIKey
COQCBADNBTZWQG-NSVAZKTRSA-N

Specifications

MW (average)
464.6630
Formula
C28H36N2O2S
CAS No.
2244781-29-9
Physical state
Other
Color
Colorless to light yellow
Shipping
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage
Liquid -20℃ 3 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO : 66.67 mg/mL

References

[1]. Mays SG, et al. Development of the First Low Nanomolar Liver Receptor Homolog-1 Agonist through Structure-guided Design. J Med Chem. 2019;62(24):11022-11034.

Same research area

Search Inflammation/Immunology

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