RapaBlock (Synonyms: ZZY05-092)

Name: RapaBlock
Brand: MedChemExpress
SKU: HY-153806
Rating: 4.5 (1 reviews)

Cat. No.: HY-153806 Purity: ≥98.0%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

RapaBlock is a potent, non-immunosuppressive and brain-impermeable FKBP12 ligand.

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

RapaBlock Chemical Structure

CAS No. : 2474076-02-1

Size	Price	Stock	Quantity
5 mg	USD 590	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 950	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1900	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 3100	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

RapaBlock is a potent, non-immunosuppressive and brain-impermeable FKBP12 ligand^[1].

In Vitro

RapaBlock appears more effective at blocking rapamycin, restoring the phospho-S6 signal to the same level as untreated cells at 100:1 stoichiometry^[1].

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

Molecular Weight

899.12

Formula

C₄₉H₇₄N₂O₁₃

CAS No.

2474076-02-1

Appearance

Solid

Color

White to off-white

SMILES

O[C@H]1[C@H](OC)C[C@@](/C=C([C@H]([C@@H]([C@@H](O)CC([C@@H](/C=C(C)/C[C@@H](C[C@H](OC)[C@]2([H])[C@@H](OC)C[C@@H](C)[C@](O)(C3=O)O2)C)CCCC4=CC=CC=[N+]4[O-])=O)C)OC([C@@]5([H])N(C3=O)CCCC5)=O)\C)([H])CC1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (111.22 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	1.1122 mL	5.5610 mL	11.1220 mL
5 mM	0.2224 mL	1.1122 mL	2.2244 mL
10 mM	0.1112 mL	0.5561 mL	1.1122 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: ≥ 2.5 mg/mL (2.78 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 (2.78 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 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 (2.78 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: ≥98.0%

Select Batch:

Data Sheet (278 KB) SDS (251 KB)

COA (262 KB) HNMR (285 KB) LCMS (146 KB)

Handling Instructions (2659 KB)

References

[1]. Ziyang Zhang, et al. Brain-restricted mTOR inhibition with binary pharmacology. Nature. 2022 Sep;609(7928):822-828. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.1122 mL	5.5610 mL	11.1220 mL	27.8050 mL
	5 mM	0.2224 mL	1.1122 mL	2.2244 mL	5.5610 mL
	10 mM	0.1112 mL	0.5561 mL	1.1122 mL	2.7805 mL
	15 mM	0.0741 mL	0.3707 mL	0.7415 mL	1.8537 mL
	20 mM	0.0556 mL	0.2780 mL	0.5561 mL	1.3902 mL
	25 mM	0.0445 mL	0.2224 mL	0.4449 mL	1.1122 mL
	30 mM	0.0371 mL	0.1854 mL	0.3707 mL	0.9268 mL
	40 mM	0.0278 mL	0.1390 mL	0.2780 mL	0.6951 mL
	50 mM	0.0222 mL	0.1112 mL	0.2224 mL	0.5561 mL
	60 mM	0.0185 mL	0.0927 mL	0.1854 mL	0.4634 mL
	80 mM	0.0139 mL	0.0695 mL	0.1390 mL	0.3476 mL
	100 mM	0.0111 mL	0.0556 mL	0.1112 mL	0.2780 mL

RapaBlock 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:

RapaBlock2474076-02-1ZZY05-092FKBPFK506-binding proteinFKBP12RapamycinInhibitorinhibitorinhibit

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RapaBlock (Synonyms: ZZY05-092)

Customer Review

RapaBlock Related Antibodies

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Biological Activity

Purity & Documentation

References

Customer Review

RapaBlock Related Antibodies

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Complete Stock Solution Preparation Table

RapaBlock Related Classifications

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