Art. -Nr.: HY-145628

CM398

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CM398 is a highly selective, orally active Sigma-2 receptor ligand with a K_i value of 0.43 nM. CM398 ameliorates age-related macular degeneration. CM398 exerts analgesic effects on visceral pain, inflammatory pain and neuropathic pain. CM398 can be used in research related to age-related macular degeneration, neuropathic pain and inflammatory pain.

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Reinheit: 99.85%
CAS. Nr.: 1121931-70-1
Formel: C₂₃H₂₉N₃O₃
Molecular Weight:395.49

Speicherung:

Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

CM398 Chemical Structure

CAS. Nr.: 1121931-70-1

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Sigma 2 Receptor

0.43 nM (Ki)

Alle Sigma Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

CM398 protects the retinal pigment epithelial cell line ARPE-19 against paraquat-induced cytotoxic damage^[1].
CM398 exhibits highly selective sub-nanomolar binding affinity (K_i = 0.43 nM) for sigma-2 receptors in rat brain homogenates, shows over 1000-fold selectivity over sigma-1 receptors, and has extremely low affinity for most non-sigma neurotransmitter receptors and transporters^[3].
CM398 undergoes rapid phase I metabolism in rat liver microsomes, with an elimination half-life of 0.10 h^[3].
CM398 (1-10 μM; 30 min) binds highly to rat plasma proteins, with an average binding rate of 93.8%^[3].

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

Parmacokinetics

Species	Dose	Route	AUC_0-t	V_d	T_1/2	CL	C_max	T_max	Bioavailability
Rat^[3]	20 mg/kg	p.o.	2733.6 ng/L.h	6.2 L/kg	1.9 h	2.2 L/h/kg	2052.8 ng/mL	0.17 h	29.0 %
Rat^[3]	1 mg/kg	i.v.	471.3 ng/L.h	5.3 L/kg	1.7 h	2.1 L/h/kg	/	/	/

In Vivo

Pretreatment with CM398 (3 mg/kg; intraperitoneal injection; single dose) partially reverses light-induced photoreceptor loss and blocks the formation of retinal autofluorescent granules in a mouse model associated with age-related macular degeneration (AMD)^[1].
CM398 (3-45 mg/kg; i.p.; single administration) produces dose-dependent analgesic effects in the mouse acetic acid writhing visceral pain model, with an i.p. ED₅₀ of 14.7 mg/kg^[2].
CM398 (0.01-30 mg/kg; intraperitoneal injection; single administration) exerts potent, dose-dependent analgesic effects in the mouse formalin inflammatory pain model, with an ED₅₀ of 0.86 mg/kg^[2].
CM398 (30 mg/kg; i.p.; single administration) exerts no significant analgesic effect in the acute thermal pain model of mouse tail-flick test at 55°C^[2].
CM398 (i.p.; single administration at doses of 10-45 mg/kg) produces time- and dose-dependent anti-allodynic effects in the mouse CCI neuropathic pain model. The efficacy of i.p. doses of 30 mg/kg and 45 mg/kg is comparable to that of gabapentin, and the duration of action is longer than that of CM-304^[2].
CM398 (i.p.; single administration, dose range 0.23-23.2 μmol/kg) exerts significant dose-dependent analgesic effects in mouse models of inflammatory pain, with statistically significant reductions in paw-licking duration observed at doses of 2.32 μmol/kg and 23.2 μmol/kg^[3].

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

Animal Model:

Abca4−/−Rdh8−/− (male, 8-10 weeks old, C57BL/6J × 129S1/SvImJ mixed background, illumination-induced retinal damage)^[1]
Dosage:

3 mg/kg
Administration:

i.p.; single injection
Result:

Restored outer nuclear layer (ONL) thickness of photoreceptors to near-basal levels compared to vehicle-treated illuminated mice.
Reduced illumination-induced retinal autofluorescent granule accumulation from 589.3 in vehicle-treated mice to fewer than 5.0.
Confirmed protective effect on photoreceptor layers via retinal histology.

Animal Model:

C57BL/6J (male, 8-12 weeks of age)^[2]
Dosage:

3 mg/kg; 10 mg/kg; 30 mg/kg; 45 mg/kg
Administration:

i.p.; single dose
Result:

Attenuated nociception in a dose-dependent manner, with an ED50 of 14.7 mg/kg, i.p.

Animal Model:

C57BL/6J (male, 8-12 weeks of age)^[2]
Dosage:

0.01 mg/kg; 0.3 mg/kg; 1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration:

i.p.; single dose
Result:

Produced significant dose-dependent antinociception (F(5,36) = 9.55, p < 0.001), with an ED50 of 0.86 mg/kg, i.p.
Resulted in significantly less paw licking compared to saline controls at doses of 3 mg/kg and 30 mg/kg, i.p. (p ≤ 0.005 or better).

Animal Model:

CD-1 (male, 8-12 weeks of age)^[2]
Dosage:

10 mg/kg; 30 mg/kg; 45 mg/kg
Administration:

i.p.; single dose
Result:

Attenuated mechanical allodynia in a time- and dose-dependent manner (factor: treatment: F(5,231) = 34.98, p < 0.001).
Produced anti-allodynic effects equivalent to gabapentin (50 mg/kg, i.p.) at all time points at doses of 30 mg/kg and 45 mg/kg, i.p. (p > 0.5 and p > 0.7, respectively).
Showed longer-lasting effects than CM-304, with significant differences from vehicle control still present at 80 minutes post-administration for 30 mg/kg (p < 0.03) and 45 mg/kg (p < 0.0001) doses.

Animal Model:

CD-1 (10-week-old male)^[3]
Dosage:

0.23 μmol/kg; 2.32 μmol/kg; 23.2 μmol/kg
Administration:

i.p.; single dose
Result:

Produced significant dose-dependent reductions in summed paw-licking duration compared to vehicle control (F(3, 24) = 7.66, p = 0.0009).

Chemical Information

CAS. Nr. 1121931-70-1
Appearance Liquid (Density: 1.166 g/cm³)
Molecular Weight 395.49
Formel C₂₃H₂₉N₃O₃
Color Light yellow to brown
SMILES

O=C1N(C)C2=C(N1CCCCN3CC4=CC(OC)=C(C=C4CC3)OC)C=CC=C2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (252.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5285 mL

12.6425 mL

25.2851 mL

5 mM

0.5057 mL

2.5285 mL

5.0570 mL

10 mM

0.2529 mL

1.2643 mL

2.5285 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 (6.32 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.32 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.32 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Mavlyutov TA, et al. Retinal Photoreceptor Protection in an AMD-Related Mouse Model by Selective Sigma-1 or Sigma-2 Receptor Modulation. Genes (Basel). 2022;13(12):2386. Published 2022 Dec 16. [Content Brief]

[2]. Wilson LL, et al. Characterization of CM-398, a Novel Selective Sigma-2 Receptor Ligand, as a Potential Therapeutic for Neuropathic Pain. Molecules. 2022;27(11):3617. Published 2022 Jun 4. [Content Brief]

[3]. Intagliata S, et al. Discovery of a highly selective sigma-2 receptor ligand, 1-(4-(6, 7-Dimethoxy-3, 4-dihydroisoquinolin-2 (1 H)-yl) butyl)-3-methyl-1 H-benzo [d] imidazol-2 (3 H)-one (CM398), with drug-like properties and antinociceptive effects in vivo[J]. The AAPS Journal, 2020, 22(5): 94.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5285 mL	12.6425 mL	25.2851 mL	63.2127 mL
	5 mM	0.5057 mL	2.5285 mL	5.0570 mL	12.6425 mL
	10 mM	0.2529 mL	1.2643 mL	2.5285 mL	6.3213 mL
	15 mM	0.1686 mL	0.8428 mL	1.6857 mL	4.2142 mL
	20 mM	0.1264 mL	0.6321 mL	1.2643 mL	3.1606 mL
	25 mM	0.1011 mL	0.5057 mL	1.0114 mL	2.5285 mL
	30 mM	0.0843 mL	0.4214 mL	0.8428 mL	2.1071 mL
	40 mM	0.0632 mL	0.3161 mL	0.6321 mL	1.5803 mL
	50 mM	0.0506 mL	0.2529 mL	0.5057 mL	1.2643 mL
	60 mM	0.0421 mL	0.2107 mL	0.4214 mL	1.0535 mL
	80 mM	0.0316 mL	0.1580 mL	0.3161 mL	0.7902 mL
	100 mM	0.0253 mL	0.1264 mL	0.2529 mL	0.6321 mL

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CM398

Orally Active Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Immunology/Inflammation Compound Library

Neuronal Signaling Compound Library

Alle Sigma Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CM398

Orally Active Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Immunology/Inflammation Compound Library

Neuronal Signaling Compound Library

Alle Sigma Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CM398 Related Classifications

HY-145628 Related Classifications