2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Calcium Channel
  4. Crisugabalin

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.

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Crisugabalin

Crisugabalin Chemical Structure

CAS No. : 2209104-84-5

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Crisugabalin Related Antibodies

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Description

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.

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.

Crisugabalin Related Antibodies
Parmacokinetics
Species Dose Route Cmax AUC0-24
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.
Molecular Weight

209.28

Formula

C12H19NO2
CAS No.
Appearance

Solid

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]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.7783 mL 23.8914 mL 47.7829 mL
5 mM 0.9557 mL 4.7783 mL 9.5566 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Purity: 99.88%

SDS (252 KB)

COA (252 KB) HNMR (324 KB) RP-HPLC (203 KB)

Handling Instructions (2659 KB)
References

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 (protect from light). 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 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 Related Classifications

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  • 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:

Crisugabalin2209104-84-5HSK16149HSK 16149HSK-16149Calcium ChannelCa2+ channelsCa channelsligand for the α2δ subunit of voltage-gated calcium channelsSprague-Dawley ratC57BL/6 miceICR micechronic painneuropathic paindiabetic neuropathyfibromyalgiainflammatory paindiabetic peripheral neuropathic painpostherpetic neuralgia
Inhibitorinhibitorinhibit

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