PeptideDB

OSBPL7-IN-1 1269826-44-9

OSBPL7-IN-1 1269826-44-9

CAS No.: 1269826-44-9

OSBPL7-IN-1 is an orally bioactive oxysterol-binding protein-like 7 (OSBPL7) inhibitor. OSBPL7-IN-1 promotes the increas
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This product is for research use only, not for human use. We do not sell to patients.

OSBPL7-IN-1 is an orally bioactive oxysterol-binding protein-like 7 (OSBPL7) inhibitor. OSBPL7-IN-1 promotes the increase of ABCA1 on the plasma membrane without affecting mRNA expression.

Physicochemical Properties


Molecular Formula C20H19CL2F3N2O3
Molecular Weight 463.28
Exact Mass 462.072
CAS # 1269826-44-9
PubChem CID 51029555
Appearance White to off-white solid powder
LogP 5.1
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 7
Rotatable Bond Count 5
Heavy Atom Count 30
Complexity 584
Defined Atom Stereocenter Count 2
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

InChi Key GYXGGHPMGUITOT-IAGOWNOFSA-N
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
Chemical Name

5-(3,4-dichlorophenyl)-N-[(1R,2R)-2-hydroxycyclohexyl]-6-(2,2,2-trifluoroethoxy)pyridine-3-carboxamide
HS Tariff Code 2934.99.9001
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)

Biological Activity


Targets OSBPL7[1] ABCA1[1]
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].
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].
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.
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.

Solubility Data


Solubility (In Vitro) DMSO: 125 mg/mL (269.82 mM)
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.