RO6806051

Cat. No.: HY-161702 Purity: 99.82%: Data Sheet
COA

SDS
Handling Instructions
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RO6806051 is a selectivity FABP4 and FABP5 inhibitor with human FABP4 K_i values of 0.011 μM and 0.23 μM, and human FABP5 K_i values of 0.086 μM and 1.17 μM. RO6806051 can be used for the research of inflammation-related diseases.

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

RO6806051 Chemical Structure

CAS No. : 1433901-75-7

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Description

In Vitro

RO6806051 acts as a potent dual inhibitor of purified human hFABP4 and hFABP5, with an ~209-fold selectivity for hFABP4 over hFABP3 and ~27-fold selectivity for hFABP5 over hFABP3^[1].
RO6806051 (10 μM) has favorable physicochemical properties, low liver microsomal clearance in human and mouse, and weak to no inhibition of major cytochrome P450 enzymes at tested concentrations^[1].
RO6806051 (10-80 μM; 24 h) exhibits significant cytotoxicity against differentiated THP-1 macrophages at concentrations of 20 μM and above^[2].
RO6806051 (5-25 μM; 18 h pre-incubation before 6 h LPS stimulation) moderately inhibits MCP-1 secretion in LPS-stimulated THP-1 macrophages at concentrations of 5, 10, and 25 μM, with the highest inhibition at 25 μM^[2].

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

Cell Viability Assay^[2]

Cell Line:	THP-1 human acute monocytic leukemia cells differentiated into macrophages
Concentration:	10-80 μM
Incubation Time:	24 h (after 24 h PMA differentiation)
Result:	Reduced cell viability of the control at 80 μM. Significantly inhibited cell viability at 20 μM.

ELISA Assay^[2]

Cell Line:	LPS-stimulated THP-1 macrophages
Concentration:	5-25 μM
Incubation Time:	18 h pre-incubation before 6 h LPS stimulation
Result:	Reduced LPS-induced MCP-1 secretion in a dose-dependent manner.

Parmacokinetics

Species	Dose	Route	CL	V_ss	Bioavailability	T_1/2
Mice^[1]	3.3 mg/kg	i.v.	5.8 mL/min/kg	3.3 L/kg	/	/
Mice^[1]	8.4 mg/kg	p.o.	/	/	99 %	5.8 h

Molecular Weight

390.87

Formula

C₂₁H₁₉ClN₆

CAS No.

1433901-75-7

Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC2=C(N=C(N3CCCCC3)C(C4=NN=NN4)=C2C5=CC=CC=C5)C=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 125 mg/mL (319.80 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	2.5584 mL	12.7920 mL	25.5840 mL
5 mM	0.5117 mL	2.5584 mL	5.1168 mL
10 mM	0.2558 mL	1.2792 mL	2.5584 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
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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

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Concentration _(final)

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In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.82%

Select Batch:

Data Sheet (279 KB) SDS (251 KB)

COA (255 KB) HNMR (257 KB) RP-HPLC (247 KB) MS (69 KB)

Handling Instructions (2659 KB)

References

[1]. Kühne H, et al. M. Design and synthesis of selective, dual fatty acid binding protein 4 and 5 inhibitors. Bioorg Med Chem Lett. 2016 Oct 15;26(20):5092-5097. [Content Brief]

[2]. He Y, et al. Discovery of Potent and Selective FABP4/5 Inhibitors with an Isoquinolone Scaffold as Potential Therapeutics for Inflammation-Related Diseases. J Med Chem. 2025;68(19):20207-20227. [Content Brief]

[3]. Chen S, et al. Recent Advances on Small-Molecule Inhibitors of Lipocalin-like Proteins. J Med Chem. 2024;67(7):5144-5167. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5584 mL	12.7920 mL	25.5840 mL	63.9599 mL
	5 mM	0.5117 mL	2.5584 mL	5.1168 mL	12.7920 mL
	10 mM	0.2558 mL	1.2792 mL	2.5584 mL	6.3960 mL
	15 mM	0.1706 mL	0.8528 mL	1.7056 mL	4.2640 mL
	20 mM	0.1279 mL	0.6396 mL	1.2792 mL	3.1980 mL
	25 mM	0.1023 mL	0.5117 mL	1.0234 mL	2.5584 mL
	30 mM	0.0853 mL	0.4264 mL	0.8528 mL	2.1320 mL
	40 mM	0.0640 mL	0.3198 mL	0.6396 mL	1.5990 mL
	50 mM	0.0512 mL	0.2558 mL	0.5117 mL	1.2792 mL
	60 mM	0.0426 mL	0.2132 mL	0.4264 mL	1.0660 mL
	80 mM	0.0320 mL	0.1599 mL	0.3198 mL	0.7995 mL
	100 mM	0.0256 mL	0.1279 mL	0.2558 mL	0.6396 mL

RO6806051 Related Classifications

Inflammation/Immunology

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:

RO68060511433901-75-7RO 6806051RO-6806051FABPFatty acid-binding proteinFABP4FABP3lipocalin domainTyr131cytochrome P450 enzymesinflammation-related diseasesTHP-1 macrophagesFABP5Arg129hERG channelInhibitorinhibitorinhibit

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RO6806051

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