2. Metabolic Enzyme/Protease
  3. Phospholipase
  4. SB-435495

SB-435495 is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM.

For research use only. We do not sell to patients.

SB-435495 Chemical Structure

SB-435495 Chemical Structure

CAS No. : 304694-39-1

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Based on 1 publication(s) in Google Scholar

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Phospholipase A PLD

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  • Purity & Documentation

  • References

  • Customer Review

Description

SB-435495 is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM[1][3].

IC50 & Target[1]

Lp-PLA2

0.06 nM (IC50)

In Vitro

SB-435495 inhibits CYP450 3A4 with an IC50 of 10 μM and the black membrane permeability is 0.017 cm/h[1].
SB-435495 (5 μM; 24 h) significantly inhibits the expression of Lp-PLA2 protein, while increases the expression levels of AMPKα and phosphorylated-AMPKα (T172) in oxLDL-exposed HUVECs[2].
SB-435495 (5 μM; 24-72 h) significantly increases cell viability and NO expression, significantly decreases ET-1 expression in the oxLDL-exposed HUVECs[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SB-435495 Related Antibodies

Western Blot Analysis[2]

Cell Line: oxLDL-exposed human umbilical vein endothelial cells
Concentration: 5 μM
Incubation Time: 24 h
Result: The expression of Lp-PLA2 protein was significantly inhibited. Increased the expression levels of AMPKα and phosphorylated-AMPKα (T172).

Cell Viability Assay[2]

Cell Line: oxLDL-exposed human umbilical vein endothelial cells
Concentration: 5 μM
Incubation Time: 24, 48 and 72 h
Result: Significantly increased cell viability.
In Vivo

SB-435495 (10 mg/kg; p.o.; once) inhibits plasma Lp-PLA2 in the WHHL rabbit[1].
SB-435495 (10 mg/kg; i.p.; daily for 28 days) effectively suppresses blood–retinal barrier (BRB) breakdown in Streptozotocin (HY-13753)-diabetic Brown Norway rats[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

720.82

Formula

C38H40F4N6O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N(CCN(CC)CC)CC1=CC=C(C2=CC=C(C(F)(F)F)C=C2)C=C1)CN(C(SCC3=CC=C(F)C=C3)=N4)C=C(CC5=CN(C)N=C5)C4=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (138.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3873 mL 6.9365 mL 13.8731 mL
5 mM 0.2775 mL 1.3873 mL 2.7746 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.80%

COA (254 KB) HNMR (316 KB) LCMS (98 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.3873 mL 6.9365 mL 13.8731 mL 34.6827 mL
5 mM 0.2775 mL 1.3873 mL 2.7746 mL 6.9365 mL
10 mM 0.1387 mL 0.6937 mL 1.3873 mL 3.4683 mL
15 mM 0.0925 mL 0.4624 mL 0.9249 mL 2.3122 mL
20 mM 0.0694 mL 0.3468 mL 0.6937 mL 1.7341 mL
25 mM 0.0555 mL 0.2775 mL 0.5549 mL 1.3873 mL
30 mM 0.0462 mL 0.2312 mL 0.4624 mL 1.1561 mL
40 mM 0.0347 mL 0.1734 mL 0.3468 mL 0.8671 mL
50 mM 0.0277 mL 0.1387 mL 0.2775 mL 0.6937 mL
60 mM 0.0231 mL 0.1156 mL 0.2312 mL 0.5780 mL
80 mM 0.0173 mL 0.0867 mL 0.1734 mL 0.4335 mL
100 mM 0.0139 mL 0.0694 mL 0.1387 mL 0.3468 mL
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SB-435495 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SB-435495304694-39-1SB435495SB 435495PhospholipaseAMPKαHUVECblood–retinal barrierorally activeInhibitorinhibitorinhibit

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