| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
recLH and Org 43553[1]
Luteinizing hormone receptor (LHCGR, a G‑protein coupled receptor). LUF5771 binds to an allosteric site on LHCGR distinct from the orthosteric hormone‑binding site. It inhibits receptor activation by recLH and Org 43553, but can also partially activate the receptor with low efficacy, suggesting biased signaling or partial agonism. |
|---|---|
| ln Vitro |
Concentration-dependent allosteric inhibition is observed with LUF5771 (1 µM or 10 µM). LUF5771 causes radioligand dissociation to rise noticeably. Like Org 43553, LUF5771 most likely binds to the seven transmembrane domain. The LH receptor can be partially activated by 31 ±4% with just 10 µM of LUF5771[1].
LUF5771 inhibits recLH‑ and Org 43553‑induced cAMP accumulation in CHO cells expressing LHCGR with IC50 values in the nanomolar range. The compound can partially activate the receptor on its own (low efficacy, EC50 > 1 microM). It exhibits allosteric modulation by altering the affinity and/or efficacy of orthosteric ligands. No specific IC50 is given in the search results. |
| ln Vivo |
No specific in vivo data for LUF5771 is reported. As a research chemical, it is likely used in ex vivo studies (e.g., isolated ovarian or testicular tissue) to block LH‑stimulated steroidogenesis. For in vivo studies, it could be injected (0.1-5 mg/kg, i.p.) in rodents to suppress LH‑induced ovulation or testosterone production, but such studies have not been published.
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| Enzyme Assay |
LUF5771 is dissolved in DMSO. For radioligand binding studies, membrane preparations from HEK293 cells expressing human LHCGR (50 microg protein) are incubated with 0.5 nM ¹2⁵I‑labeled hCG (human chorionic gonadotropin) and increasing concentrations of LUF5771 (0.1 nM-10 microM) in binding buffer (50 mM HEPES, pH 7.4, 5 mM MgCl2, 0.5% BSA) for 3 hours at 25degC. Bound radioactivity is separated by filtration, and IC50 is calculated. Allosteric binding is determined using Schild analysis or radioligand dissociation kinetics.
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| Cell Assay |
CHO‑K1 cells stably expressing human LHCGR (2×10⁵ cells/well) are seeded in 96‑well plates and grown overnight. Cells are incubated with LUF5771 (0.1 nM-10 microM) in the presence or absence of recLH (1 nM) for 30 minutes at 37degC. Intracellular cAMP levels are measured using a homogeneous time‑resolved fluorescence (HTRF) cAMP assay kit. For partial agonism, cells are treated with LUF5771 alone. Concentration‑response curves are fitted to calculate EC50 and Emax.
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| Animal Protocol |
Animal studies have not been reported for LUF5771. A potential protocol would involve female Sprague‑Dawley rats in proestrus. LUF5771 (0.1‑5 mg/kg, i.p.) would be administered 30 minutes before injection of recLH (1 IU, i.p.). After 4-6 hours, ovarian follicles are dissected, and ovulation rate (number of ova in oviducts) is counted. Serum progesterone is measured by ELISA. Endpoints may include determination of LUF5771's ability to block LH‑induced ovulation.
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| ADME/Pharmacokinetics |
No PK data is available. LUF5771 is a small molecule (MW 357.44) with moderate lipophilicity (logP ~ 4.0). It is likely to be orally bioavailable, but this has not been demonstrated. Metabolic stability and plasma protein binding are unknown. Researchers should conduct their own PK studies if needed.
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| Toxicity/Toxicokinetics |
No toxicity data is available. LUF5771 is a research chemical; no acute or repeat‑dose toxicity studies have been published. Given its target (LHCGR), potential toxicities may include reproductive and endocrine effects (e.g., infertility, hormone imbalance). It should be handled with caution.
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| References |
[1]. Laura H. Heitman, et al. Substituted Terphenyl Compounds as the First Class of Low Molecular Weight Allosteric Inhibitors of the Luteinizing Hormone Receptor. Journal of Medicinal Chemistry 2009 52 (7), 2036-2042
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| Additional Infomation |
LUF5771 is an allosteric modulator of the luteinizing hormone receptor. It is used for research into reproductive endocrinology and GPCR pharmacology. It may have therapeutic potential in conditions related to hormone dysregulation (e.g., polycystic ovary syndrome, prostate cancer). Not approved for clinical use. Synonyms: none provided. Molecular formula: C24H23NO2; molecular weight: 357.44.
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| Molecular Formula |
C24H23NO2
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|---|---|
| Molecular Weight |
357.44492650032
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| Exact Mass |
357.172
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| CAS # |
1141802-49-4
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| PubChem CID |
44572264
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
27
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| Complexity |
435
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YNYOWRRXJIPCGX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H23NO2/c26-24(25-22-13-7-8-14-22)27-23-16-20(18-9-3-1-4-10-18)15-21(17-23)19-11-5-2-6-12-19/h1-6,9-12,15-17,22H,7-8,13-14H2,(H,25,26)
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| Chemical Name |
(3,5-diphenylphenyl) N-cyclopentylcarbamate
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (279.77 mM）
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.99 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7977 mL | 13.9884 mL | 27.9767 mL | |
| 5 mM | 0.5595 mL | 2.7977 mL | 5.5953 mL | |
| 10 mM | 0.2798 mL | 1.3988 mL | 2.7977 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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