Cat. No.: HY-142240

Crisugabalin

(Synonyms: HSK16149)

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Crisugabalin is an orally active, selective ligand for the α2δ subunit of voltage-gated calcium channels, with a target IC₅₀ of 3.96 nM in rats. Crisugabalin inhibits the binding of [³H]gabapentin to the α2δ subunit, reduces calcium influx, decreases neuronal excitability, and impairs nociceptive transmission. Crisugabalin alleviates mechanical allodynia, neuropathic pain and inflammatory pain in rats, and reduces phase II pain behaviors. Crisugabalin can be used in research related to chronic pain, neuropathic pain, diabetic neuropathy, fibromyalgia, inflammatory pain, diabetic peripheral neuropathy and postherpetic neuralgia.

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

Purity: 99.88%
CAS No.: 2209104-84-5
Formula: C₁₂H₁₉NO₂
Molecular Weight:209.28

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Crisugabalin Chemical Structure

CAS No.: 2209104-84-5

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All Calcium Channel Isoforms :

In Vitro

Crisugabalin (incubated at 25 °C for 30 min) potently binds to the VGCC α₂δ subunit in the cerebral cortex cell membranes of Wistar rats, with an IC₅₀ of 3.96 nM^[1].

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

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-24
Rat^[1]	1 mg/kg	p.o.	0.69 μg/mL	1.46 μg·h/mL
Rat^[1]	3 mg/kg	p.o.	1.69 μg/mL	4.27 μg·h/mL
Rat^[1]	10 mg/kg	p.o.	6.13 μg/mL	15.41 μg·h/mL
Rat^[1]	30 mg/kg	p.o.	16.90 μg/mL	61.63 μg·h/mL

In Vivo

Crisugabalin (1-30 mg/kg; p.o.; single administration) dose-dependently increases the mechanical pain threshold in rats with CCI-induced neuropathic pain^[1].
Crisugabalin (1-30 mg/kg; p.o.; single administration) dose-dependently increases the mechanical pain threshold in streptozotocin (HY-13753)-induced diabetic neuropathy rats^[1].
Crisugabalin (p.o.; single administration; 30 mg/kg) inhibits intermittent cold stress (ICS)-induced mechanical hyperalgesia in fibromyalgia mice^[1].
Crisugabalin (10-30 mg/kg; p.o.; single administration) dose-dependently alleviates formalin-induced phase II inflammatory pain behaviors^[1].
Crisugabalin (100 mg/kg; p.o.; single administration) induces sedative effects in rats^[1].

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

Animal Model:

Sprague-Dawley (male, 160-180 g, CCI-induced neuropathic pain)^[1]
Dosage:

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

p.o.; single dose
Result:

Increased 50% PWT to 3.24-fold that of vehicle controls at 2 hours post-dosing (30 mg/kg, P < 0.001), with effects peaking at 6 hours post-dosing.
Produced PWT values of 12.93 g and 13.66 g at 2 and 4 hours post-dosing, respectively (10 mg/kg), similar to the 30 mg/kg group (11.93 g, 13.55 g).
Had a lower PWT than the 30 mg/kg group at 6 hours post-dosing (10 mg/kg) but efficacy comparable to 30 mg/kg pregabalin.
Significantly increased 50% PWT to 7.33 g vs.
3.11 g in vehicle controls at 4 hours post-dosing (3 mg/kg).
Had a minimum effective dose (MED) of 10 mg/kg for increased AUC of 50% PWT vs.
time.

Animal Model:

Sprague-Dawley (male, 160-180 g, STZ-induced diabetic neuropathy)^[1]
Dosage:

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

p.o.; single dose
Result:

Significantly increased 50% PWT at 2 hours post-dosing (30 mg/kg), with efficacy persisting up to 24 hours post-dosing.
Increased 50% PWT to 2.4-fold at 2 hours post-dosing (10 mg/kg), with significant increases at 4 hours (10.55 g vs.
4.35 g) and 6 hours (11.74 g vs.
4.24 g), and efficacy persisting up to 8 hours post-dosing.
Doubled PWT vs.
vehicle controls at 6 hours post-dosing (3 mg/kg).
Had a MED of 10 mg/kg for increased AUC of 50% PWT vs.
time, with efficacy at 10 mg/kg comparable to 30 mg/kg pregabalin.

Animal Model:

C57BL/6 (male, 18-25 g, ICS-induced fibromyalgia)^[1]
Dosage:

30 mg/kg
Administration:

p.o.; single dose
Result:

Had a MED of 30 mg/kg for increased 50% PWT.
Induced a 2.6-fold increase in 50% PWT, with efficacy comparable to 30 mg/kg pregabalin.

Animal Model:

ICR (male, 25-35 g, formalin-induced inflammatory pain)^[1]
Dosage:

10 mg/kg; 30 mg/kg
Administration:

p.o.; single dose
Result:

Decreased formalin-induced phase II nociceptive motion counts in a dose-dependent manner.
Produced a 1.6-fold and 2.2-fold decrease in phase II motion counts vs.
vehicle controls at 10 mg/kg and 30 mg/kg, respectively.
Had efficacy at 30 mg/kg comparable to 30 mg/kg pregabalin.
Had no significant effect on phase I motion counts at 30 mg/kg.

Animal Model:

Sprague-Dawley (male, 160-180 g)^[1]
Dosage:

100 mg/kg
Administration:

p.o.; single dose
Result:

Produced a 3-fold decrease in total distance traveled vs.
vehicle controls.
Had a MED of 100 mg/kg for sedative effects, with efficacy comparable to 100 mg/kg pregabalin.

Chemical Information

CAS No. 2209104-84-5
Appearance Solid
Molecular Weight 209.28
Formula C₁₂H₁₉NO₂
Color White to off-white
SMILES

O=C(O)C[C@@]1(CN)[C@](C2)([H])[C@@]3([H])C[C@]2([H])CC[C@@]13[H]
Synonyms

HSK16149
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

DMSO : ≥ 100 mg/mL (477.83 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.7783 mL

23.8914 mL

47.7829 mL

5 mM

0.9557 mL

4.7783 mL

9.5566 mL

10 mM

0.4778 mL

2.3891 mL

4.7783 mL

Molarity Calculator

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

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)

References

[1]. Gou X, et al. Pharmacology and Mechanism of Action of HSK16149, a Selective Ligand of α2δ Subunit of Voltage-Gated Calcium Channel with Analgesic Activity in Animal Models of Chronic Pain. J Pharmacol Exp Ther. 2021 Mar;376(3):330-337. [Content Brief]

[2]. Wang Z, et al. Quantification of crisugabalin (HSK16149) in biological matrix by LC-MS/MS method: An application to rat pharmacokinetic and tissue distribution studies. J Chromatogr B Analyt Technol Biomed Life Sci. 2025;1251:124396. [Content Brief]

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.7783 mL	23.8914 mL	47.7829 mL	119.4572 mL
	5 mM	0.9557 mL	4.7783 mL	9.5566 mL	23.8914 mL
	10 mM	0.4778 mL	2.3891 mL	4.7783 mL	11.9457 mL
	15 mM	0.3186 mL	1.5928 mL	3.1855 mL	7.9638 mL
	20 mM	0.2389 mL	1.1946 mL	2.3891 mL	5.9729 mL
	25 mM	0.1911 mL	0.9557 mL	1.9113 mL	4.7783 mL
	30 mM	0.1593 mL	0.7964 mL	1.5928 mL	3.9819 mL
	40 mM	0.1195 mL	0.5973 mL	1.1946 mL	2.9864 mL
	50 mM	0.0956 mL	0.4778 mL	0.9557 mL	2.3891 mL
	60 mM	0.0796 mL	0.3982 mL	0.7964 mL	1.9910 mL
	80 mM	0.0597 mL	0.2986 mL	0.5973 mL	1.4932 mL
	100 mM	0.0478 mL	0.2389 mL	0.4778 mL	1.1946 mL

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Crisugabalin

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All Calcium Channel Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Crisugabalin

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Anti-diabetic Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Neuroprotective Compound Library

Mechanoreceptors Compound Library

Calcium Channel Blocker Library

Antihypertensive Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

All Calcium Channel Isoforms

Biological Activity

Chemical Information

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Crisugabalin Related Classifications

HY-142240 Related Classifications