Olorinab (Synonyms: APD 371)

Name: Olorinab
Brand: MedChemExpress
SKU: HY-111110
Rating: 4.5 (1 reviews)

Cat. No.: HY-111110 Purity: 99.29%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB₂) agonist, with an EC₅₀ of 6.2 nM for hCB₂.

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

Olorinab Chemical Structure

CAS No. : 1268881-20-4

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 150	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 240	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 480	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 780	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1250	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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CB1 CB2

Biological Activity
Purity & Documentation
References
Customer Review

Description

Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB₂) agonist, with an EC₅₀ of 6.2 nM for hCB₂.

IC₅₀ & Target

EC50: 6.2 nM (hCB₂)^[1].

In Vitro

A comprehensive in vitro profile of Olorinab (APD 371) (6) shows that single digit nanomolar potency and full intrinsic efficacy are maintained in all species assessed, and that Olorinab (APD 371) is highly selective for CB₂ over CB₁ in both binding and functional assays. Furthermore, Olorinab (APD 371) induces efficient receptor internalization (~106% relative to the CB1/2 agonist CP55,940) in CHO cells expressing HA-tagged rat CB₂ suggesting that, according to the hypothesis, Olorinab (APD 371) would be able to drive agonist-induced receptor recycling^[1].

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

In Vivo

Olorinab (APD 371) significantly increases paw withdrawal thresholds at doses ≥3 mg/kg PO (ED₅₀=2.3 mg/kg). In a separate experiment, a single dose of Olorinab (APD 371) (10 mg/kg, PO) inhibits paw withdrawal threshold for up to 4 hours after administration. Seperately, the analgesic effects of Olorinab (APD 371) are shown to be highly likely mediated via activity at CB₂ receptors^[1].

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

Clinical Trial

Molecular Weight

357.41

Formula

C₁₈H₂₃N₅O₃

CAS No.

1268881-20-4

Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=NN(C2=C[N+]([O-])=CC=N2)C3=C1C[C@@]4([H])[C@]3([H])C4)N[C@H](CO)C(C)(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°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 : 200 mg/mL (559.58 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	2.7979 mL	13.9895 mL	27.9791 mL
5 mM	0.5596 mL	2.7979 mL	5.5958 mL
10 mM	0.2798 mL	1.3990 mL	2.7979 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:

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: ≥ 5 mg/mL (13.99 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (13.99 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (13.99 mM); Clear solution

This protocol yields a clear solution of ≥ 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 (50.0 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.29%

Select Batch:

Data Sheet (279 KB) SDS (252 KB)

COA (259 KB) LCMS (93 KB) Elemental Analysis Report (116 KB)

Handling Instructions (2659 KB)

References

[1]. Han S, et al. Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain. ACS Med Chem Lett. 2017 Nov 30;8(12):1309-1313. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.7979 mL	13.9895 mL	27.9791 mL	69.9477 mL
	5 mM	0.5596 mL	2.7979 mL	5.5958 mL	13.9895 mL
	10 mM	0.2798 mL	1.3990 mL	2.7979 mL	6.9948 mL
	15 mM	0.1865 mL	0.9326 mL	1.8653 mL	4.6632 mL
	20 mM	0.1399 mL	0.6995 mL	1.3990 mL	3.4974 mL
	25 mM	0.1119 mL	0.5596 mL	1.1192 mL	2.7979 mL
	30 mM	0.0933 mL	0.4663 mL	0.9326 mL	2.3316 mL
	40 mM	0.0699 mL	0.3497 mL	0.6995 mL	1.7487 mL
	50 mM	0.0560 mL	0.2798 mL	0.5596 mL	1.3990 mL
	60 mM	0.0466 mL	0.2332 mL	0.4663 mL	1.1658 mL
	80 mM	0.0350 mL	0.1749 mL	0.3497 mL	0.8743 mL
	100 mM	0.0280 mL	0.1399 mL	0.2798 mL	0.6995 mL

Olorinab Related Classifications

Neurological 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:

Olorinab1268881-20-4APD 371APD371APD-371Cannabinoid ReceptorInhibitorinhibitorinhibit

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Olorinab (Synonyms: APD 371)

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Olorinab Related Antibodies

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Complete Stock Solution Preparation Table

Olorinab Related Classifications

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