MRT-83

Name: MRT-83
Brand: MedChemExpress
SKU: HY-18287
Rating: 4.5 (1 reviews)

Cat. No.: HY-18287 Purity: 99.27%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

MRT-83 is a potent antagonist of Smo, with an IC₅₀ in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.

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

MRT-83 Chemical Structure

CAS No. : 1263131-92-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 142	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 142	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 390	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 670	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1150	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 MRT-83:

MRT-83 hydrochloride Get quote

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Biological Activity
Protocol
Purity & Documentation
References
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Description

MRT-83 is a potent antagonist of Smo, with an IC₅₀ in the nanomolar range. MRT-83 also blocks Hedgehog (Hh) signaling.

IC₅₀ & Target

Smo^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
C3H 10T1/2	IC₅₀	0.011 μM Compound: 86	Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs Inhibition of SAG-induced differentiation of mouse mesenchymal pluripotent C3H10T1/2 cells to alkaline phosphatase positive oeseoblasts after 6 hrs	[PMID: 22268551]
HEK293	IC₅₀	5 nM Compound: 86	Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy Displacement of BODIPY-labelled cyclopamine from human Smo receptor expressed in HEK293 cells after 2 hrs by fluorescence microscopy	[PMID: 22268551]
Shh Light II	IC₅₀	0.015 μM Compound: 86	Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay Inhibition of Smo-mediated Hh signaling in human Shh-light2 cells by luciferase reporter gene assay	[PMID: 22268551]

In Vitro

MRT-83 displays full antagonist properties with an IC₅₀ (~3 nM) for inhibiting ShhN (3 nM)-induced proliferation of rat GCPs. MRT-83 also blocks SAG (0.01 μM)-induced proliferation of GCPs (IC₅₀ ~6 nM). MRT-83 blocks BC binding to HEK-hSmo cells in a dose-dependent manner with an IC₅₀ of 4.6 nM. MRT-83 abrogates BC binding to cells expressing mouse Smo with an IC₅₀ of 14 nM, which is in good correlation with its IC₅₀ in the Shh-light2 and alkaline phosphatase assays^[1].

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

In Vivo

Animals treated with ShhN in the presence of MRT-83 are as healthy as those of the other groups but up-regulation of Ptc transcription in the SVZ of these animals is no longer observed in agreement with a complete inhibition of ShhN-mediated effects (8.7±2.4 Ptc⁺ cells/section, n=9) and is not different from vehicle-mediated effects. MRT-83 but not MRT-36 antagonizes the up-regulation of Ptc transcription induced by ShhN in vivo in the SVZ of the LV^[1].

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

Molecular Weight

538.59

Formula

C₃₁H₃₀N₄O₅

CAS No.

1263131-92-5

Appearance

Solid

Color

White to light yellow

SMILES

COC1=C(OC)C(OC)=CC(C(NC(NC2=CC(NC(C3=CC=C(C4=CC=CC=C4)C=C3)=O)=C(C)C=C2)=N)=O)=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 : 250 mg/mL (464.17 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	1.8567 mL	9.2835 mL	18.5670 mL
5 mM	0.3713 mL	1.8567 mL	3.7134 mL
10 mM	0.1857 mL	0.9283 mL	1.8567 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
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: ≥ 2.08 mg/mL (3.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.86 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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: 99.27%

Select Batch:

Data Sheet (272 KB) SDS (393 KB)

COA (246 KB) HNMR (286 KB) LCMS (97 KB)

Handling Instructions (2659 KB)

References

[1]. Roudaut H, et al. Identification and mechanism of action of the acylguanidine MRT-83, a novel potent Smoothened antagonist. Mol Pharmacol. 2011 Mar;79(3):453-60. [Content Brief]

Animal Administration
^[1]

Mice^[1]
Four groups of six animals received 5 μL of 45% 2-hydroxypropyl-β-cyclodextrin PBS solution containing 0.9 μg of ShhN alone or in the presence of MRT-83 (200 ng) or MRT-36 (110 ng). A control group receive 5 μL of 45% 2-hydroxypropyl-β-cyclodextrin solution alone. All groups are analyzed 48 h after the injection^[1]

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

References

[1]. Roudaut H, et al. Identification and mechanism of action of the acylguanidine MRT-83, a novel potent Smoothened antagonist. Mol Pharmacol. 2011 Mar;79(3):453-60. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.8567 mL	9.2835 mL	18.5670 mL	46.4175 mL
	5 mM	0.3713 mL	1.8567 mL	3.7134 mL	9.2835 mL
	10 mM	0.1857 mL	0.9283 mL	1.8567 mL	4.6417 mL
	15 mM	0.1238 mL	0.6189 mL	1.2378 mL	3.0945 mL
	20 mM	0.0928 mL	0.4642 mL	0.9283 mL	2.3209 mL
	25 mM	0.0743 mL	0.3713 mL	0.7427 mL	1.8567 mL
	30 mM	0.0619 mL	0.3094 mL	0.6189 mL	1.5472 mL
	40 mM	0.0464 mL	0.2321 mL	0.4642 mL	1.1604 mL
	50 mM	0.0371 mL	0.1857 mL	0.3713 mL	0.9283 mL
	60 mM	0.0309 mL	0.1547 mL	0.3094 mL	0.7736 mL
	80 mM	0.0232 mL	0.1160 mL	0.2321 mL	0.5802 mL
	100 mM	0.0186 mL	0.0928 mL	0.1857 mL	0.4642 mL

MRT-83 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:

MRT-831263131-92-5MRT83MRT 83SmoSmoothenedInhibitorinhibitorinhibit

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MRT-83

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Complete Stock Solution Preparation Table

MRT-83 Related Classifications

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