[CAS NO. 68682-01-9] (2R/S)-6-PNG
PRODUCTS SPECIFICATIONS [68682-01-9]
DESCRIPTION [68682-01-9]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 340.37 |
| Molecular Formula | C20H20O5 |
| SMILES | O=C1CC(C2=CC=C(O)C=C2)OC3=CC(O)=C(C/C=C(C)\C)C(O)=C13 |
Summary
(2R/S)-6-PNG (6-Prenylnaringenin) is a potent and reversible Ca v 3.2 T-type Ca 2+ channels (T-channels) blocker. (2R/S)-6-PNG can penetrate the blood-brain barrier (BBB). (2R/S)-6-PNG suppresses neuropathic and visceral pain in mice [1] .
IC50 & Target
|
T-type calcium channel |
In Vitro
(2R/S)-6-PNG (6-Prenylnaringenin) potently blocks Ca
v
3.2, but exhibits minor effect on high-voltage-activated Ca
2+
channels and voltage-gated Na
+
channels in differentiated NG108-15 cells
[1]
.
On the basis of IC50 values, the proportion (Ca
v
3.2/HVA) of the inhibition potency of (2R/S)-6-PNG on Ca
v
3.2 and HVA-currents is 5.20, and that (Ca
v
3.2/Na
v
) on Ca
v
3.2 and Na
v
-currents is 3.54
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
(2R/S)-6-PNG (6-Prenylnaringenin; 10-30 mg/kg; i.p.; single dose; 15 min before Na2S) significantly reduced the Na
2
S-induced nociceptive behavior and/or referred hyperalgesia in onscious mice with intracolonic (i.col.) administration of Na
2
S, an H
2
S donor
[1]
.
(2R/S)-6-PNG (30 mg/kg; i.p.) prevents the increased number of phosphorylated ERK-positive cells following i.col. Na2S in laminae I-II, V-VI and X to which the primary afferent neurons project, and the Na2S-induced increase in the phosphorylated ERK-positive cell number
[1]
.
(2R/S)-6-PNG (0.01-1 and 0.1-10 nmol/paw; intraplantar administration) restores the mechanical allodynia induced by partial sciatic nerve ligation (PSNL) and by i.p. administration of Oxaliplatin (OHP) a, respectively, in a dose-dependent manner
[1]
.
(2R/S)-6-PNG (20-30 mg/kg; i.p.) significantly reverses the PSNL-induced allodynia. (2R/S)-6-PNG (10-20 mg/kg; i.p.) significantly reverses the OHP-induced allodynia (5 mg/kg; i.p.; single dose)
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT03140397 | University of Hohenheim|Universität Tübingen |
Safety After Oral Intake|Pharmacokinetics After Oral Intake|Immune Cells Activity
|
January 2016 | Early Phase 1 |
| NCT03286777 | University of Hohenheim|Universität Tübingen |
Safety of Native vs. Micellar 6-PN After Oral Intake|Pharmacokinetics of Native vs. Micellar 6-PN After Oral Intake|PBMC Activity After Native vs. Micellar 6-PN Oral Intake
|
June 22, 2017 | Not Applicable |
Appearance
Solid
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
DMSO : 125 mg/mL ( 367.25 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.9380 mL | 14.6899 mL | 29.3798 mL |
| 5 mM | 0.5876 mL | 2.9380 mL | 5.8760 mL |
| 10 mM | 0.2938 mL | 1.4690 mL | 2.9380 mL |