| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
OSBPL7[1] ABCA1[1]
The primary target of OSBPL7-IN-1 is OSBPL7, an oxysterol-binding protein. By inhibiting OSBPL7, the compound increases the localization of the ATP-binding cassette transporter ABCA1 at the plasma membrane. This facilitates cholesterol efflux, which is important for maintaining cellular lipid homeostasis. |
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| ln Vitro |
In human podocytes cultivated in vitro, OSBPL7-IN-1 (compound G or Cpd G; 1-10 µM) increases the plasma membrane ATP-binding cassette transporter (ABCA1) and dramatically increases ABCA1-dependent cholesterol efflux[1].
In vitro, OSBPL7-IN-1 (1-10 µM) increases plasma membrane ABCA1 in cultured human podocytes and significantly increases ABCA1-dependent cholesterol efflux. It shows low nanomolar CB1R binding affinity (Ki = 13 nM) while preserving OSBPL7 target engagement. |
| ln Vivo |
In animal models of proteinuric kidney illness, therapy with OSBPL7-IN-1 (100 mg/kg; oral gavage; daily; for 28 days) normalizes proteinuria and avoids the deterioration of renal function[1].
In vivo, OSBPL7-IN-1 (100 mg/kg; oral gavage; once daily; for 28 days) normalizes proteinuria and prevents renal function decline in mouse models of proteinuric kidney disease. Its oral bioavailability and efficacy make it a promising candidate for kidney disease research. |
| Enzyme Assay |
Non-cellular assays for OSBPL7-IN-1 typically involve measuring its binding affinity to OSBPL7 using surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). Its ability to inhibit OSBPL7 activity can be assessed using biochemical assays.
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| Cell Assay |
Cellular assays for OSBPL7-IN-1 are conducted using podocytes or other cell lines. Cells are treated with the compound, and ABCA1 localization at the plasma membrane is assessed by immunofluorescence or cell surface biotinylation. Cholesterol efflux is measured using labeled cholesterol.
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| Animal Protocol |
Animal/Disease Models: Female balb/c (Bagg ALBino) mouse induced by Adriamycin (ADR)[1]
Doses: 100 mg/kg Route of Administration: Oral gavage; daily; for 28 days Experimental Results: Normalized proteinuria, and Dramatically decreased renal fibrosis and renal functional decline. In vivo animal experiments for OSBPL7-IN-1 are conducted in mouse models of proteinuric kidney disease. The compound is administered orally, and its effects on proteinuria, renal function, and kidney histology are assessed. ABCA1 expression and cholesterol efflux are measured in kidney tissues. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of OSBPL7-IN-1 indicate that it is orally active. Its absorption, distribution, metabolism, and excretion have been characterized in preclinical studies, supporting its use in animal models of kidney disease.
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| Toxicity/Toxicokinetics |
Toxicological data for OSBPL7-IN-1 are limited, as it is a research compound. It is for research use only. Standard laboratory safety precautions should be followed when handling the compound.
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| References |
[1]. Matthew B Wright, et al. Compounds targeting OSBPL7 increase ABCA1-dependent cholesterol efflux preserving kidney function in two models of kidney disease. Nat Commun. 2021 Aug 2;12(1):4662.
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| Additional Infomation |
OSBPL7-IN-1 is a first-in-class, orally active inhibitor of OSBPL7. It is a valuable research tool for studying the role of OSBPL7 and ABCA1 in cholesterol metabolism and kidney disease. Its ability to prevent renal function decline highlights its therapeutic potential for proteinuric kidney diseases.
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| Molecular Formula |
C20H19CL2F3N2O3
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|---|---|
| Molecular Weight |
463.28
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| Exact Mass |
462.072
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| CAS # |
1269826-44-9
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| PubChem CID |
51029555
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| Appearance |
White to off-white solid powder
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| LogP |
5.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
30
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| Complexity |
584
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1CC[C@H]([C@@H](C1)NC(=O)C2=CC(=C(N=C2)OCC(F)(F)F)C3=CC(=C(C=C3)Cl)Cl)O
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| InChi Key |
GYXGGHPMGUITOT-IAGOWNOFSA-N
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| InChi Code |
InChI=1S/C20H19Cl2F3N2O3/c21-14-6-5-11(8-15(14)22)13-7-12(9-26-19(13)30-10-20(23,24)25)18(29)27-16-3-1-2-4-17(16)28/h5-9,16-17,28H,1-4,10H2,(H,27,29)/t16-,17-/m1/s1
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| Chemical Name |
5-(3,4-dichlorophenyl)-N-[(1R,2R)-2-hydroxycyclohexyl]-6-(2,2,2-trifluoroethoxy)pyridine-3-carboxamide
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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: 125 mg/mL (269.82 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.49 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 20.8 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 | 2.1585 mL | 10.7926 mL | 21.5852 mL | |
| 5 mM | 0.4317 mL | 2.1585 mL | 4.3170 mL | |
| 10 mM | 0.2159 mL | 1.0793 mL | 2.1585 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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