SB-435495

Name: SB-435495
Brand: MedChemExpress
SKU: HY-19415
Rating: 4.5 (1 reviews)

Cat. No.: HY-19415 Purity: 99.80%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 304694-39-1

Size	Price	Stock	Quantity
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 250	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 550	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 900	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1450	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of SB-435495:

SB-435495 hydrochloride Get quote
SB-435495 ditartrate Get quote

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Phospholipase A PLD Phospholipase C

Biological Activity
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.

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.

304694-39-1

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
10 mM	0.1387 mL	0.6937 mL	1.3873 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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%

Select Batch:

Data Sheet (278 KB) SDS (251 KB)

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

Handling Instructions (2659 KB)

References

[1]. Blackie JA, et al. The discovery of SB-435495. A potent, orally active inhibitor of lipoprotein-associated phospholipase A(2) for evaluation in man. Bioorg Med Chem Lett. 2002 Sep 16;12(18):2603-6. [Content Brief]

[2]. Yang L, et al. AMP-activated protein kinase mediates the effects of lipoprotein-associated phospholipase A2 on endothelial dysfunction in atherosclerosis. Exp Ther Med. 2017 Apr;13(4):1622-1629. [Content Brief]

[3]. Canning P, et al. Lipoprotein-associated phospholipase A2 (Lp-PLA2) as a therapeutic target to prevent retinal vasopermeability during diabetes. Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7213-8. [Content Brief]

Complete Stock Solution Preparation Table

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

SB-435495 Related Classifications

Metabolic Disease

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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Complete Stock Solution Preparation Table

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