Dalcetrapib (Synonyms: JTT-705; RO4607381)

Name: Dalcetrapib
Brand: MedChemExpress
SKU: HY-14950
Rating: 4.5 (1 reviews)

Cat. No.: HY-14950 Purity: 99.19%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Dalcetrapib (JTT-705) is an orally active cholesteryl ester transfer protein (CETP) inhibitor with IC₅₀s of 204.6 nM and 6 μM against recombinant human (rh) CETP and human plasma CETP, respectively.

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

Dalcetrapib Chemical Structure

CAS No. : 211513-37-0

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 286	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 286	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 80	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 200	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
250 mg	USD 800	In-stock	Estimated Time of Arrival: December 31
500 mg		Get quote
1 g		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

IC₅₀ & Target

IC₅₀: 204.6 nM (rhCETP)^[1], 6 μM (human plasma CETP)^[2]

In Vitro

Dalcetrapib (JTT-705) (0.1-10 μM; 21 h) dose-dependently increases pre-β-HDL formation^[1].
Dalcetrapib (0-30 μM; 24 h) inhibits the CETP activity of media in HepG2 in a dose-dependent manner^[3].

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

In Vivo

Dalcetrapib (JTT-705) (30 or 100 mg/kg; p.o.; once a day for 3 days) increases plasma HDL cholesterol in rabbits^[2].
Dalcetrapib (100 mg/kg; i.g.; twice daily for 7 days) significantly increases fecal elimination of neutral sterols, bile acids, and plasma HDL-cholesterol^[1].

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

Animal Model:	Male JW rabbits^[2]
Dosage:	30 or 100 mg/kg
Administration:	Oral administration, once a day for 3 days
Result:	Increased plasma HDL cholesterol by 27% and 54% at 30 mg/kg and 100 mg/kg, respectively.

Clinical Trial

Molecular Weight

389.59

Formula

C₂₃H₃₅NO₂S

CAS No.

211513-37-0

Appearance

Solid

Color

White to off-white

SMILES

CC(C)C(SC1=C(NC(C2(CC(CC)CC)CCCCC2)=O)C=CC=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (128.34 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5668 mL	12.8340 mL	25.6680 mL
5 mM	0.5134 mL	2.5668 mL	5.1336 mL
10 mM	0.2567 mL	1.2834 mL	2.5668 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.42 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.42 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.19%

Select Batch:

Data Sheet (273 KB) SDS (393 KB)

COA (247 KB) HNMR (183 KB) LCMS (508 KB)

Handling Instructions (2659 KB)

References

[1]. Niesor EJ, et al. Modulating cholesteryl ester transfer protein activity maintains efficient pre-β-HDL formation and increases reverse cholesterol transport. J Lipid Res. 2010, 51(12), 3443-3454. [Content Brief]

[2]. Shinkai H, et al. J Med Chem. bis(2-(Acylamino)phenyl) disulfides, 2-(acylamino)benzenethiols, and S-(2-(acylamino)phenyl) alkanethioates as novel inhibitors of cholesteryl ester transfer protein. 2000, 43(19), 3566-3572. [Content Brief]

[3]. Huang Z, et al. Dual effects on HDL metabolism by cholesteryl ester transfer protein inhibition in HepG2 cells. Am J Physiol Endocrinol Metab. 2003, 284(6), E1210-E1219. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.5668 mL	12.8340 mL	25.6680 mL	64.1700 mL
	5 mM	0.5134 mL	2.5668 mL	5.1336 mL	12.8340 mL
	10 mM	0.2567 mL	1.2834 mL	2.5668 mL	6.4170 mL
	15 mM	0.1711 mL	0.8556 mL	1.7112 mL	4.2780 mL
	20 mM	0.1283 mL	0.6417 mL	1.2834 mL	3.2085 mL
	25 mM	0.1027 mL	0.5134 mL	1.0267 mL	2.5668 mL
	30 mM	0.0856 mL	0.4278 mL	0.8556 mL	2.1390 mL
	40 mM	0.0642 mL	0.3209 mL	0.6417 mL	1.6043 mL
	50 mM	0.0513 mL	0.2567 mL	0.5134 mL	1.2834 mL
	60 mM	0.0428 mL	0.2139 mL	0.4278 mL	1.0695 mL
	80 mM	0.0321 mL	0.1604 mL	0.3209 mL	0.8021 mL
	100 mM	0.0257 mL	0.1283 mL	0.2567 mL	0.6417 mL

Dalcetrapib 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:

Dalcetrapib211513-37-0JTT-705 RO4607381JTT705JTT 705RO4607381RO 4607381RO-4607381CETPCholesteryl ester transfer proteinorally activepre-β-HDLHDL cholesterolInhibitorinhibitorinhibit

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Dalcetrapib (Synonyms: JTT-705; RO4607381)

Customer Review

Dalcetrapib Related Antibodies

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•Related Screening Libraries:

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Biological Activity

Purity & Documentation

References

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Dalcetrapib Related Antibodies

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Complete Stock Solution Preparation Table

Dalcetrapib Related Classifications

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