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RN-1747

Cat. No. M8129
RN-1747 Structure
Size Price Availability Quantity
5mg USD 77  USD77 In stock
10mg USD 140  USD140 In stock
25mg USD 270  USD270 In stock
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Quality Control & Documentation
Biological Activity

TRPV4, a close relative of the vanilloid receptor TRPV1, is activated by diverse modalities such as endogenous lipid ligands, hypotonicity, protein kinases and, possibly, mechanical inputs. TRPV4 is a nociceptor playing an important role in inflammatory and neuropathic mechanical hyperalgesia in rodent models apparently specifically activated under pathological conditions.

Chemical Information
Molecular Weight 395.86
Formula C17H18ClN3O4S
CAS Number 1024448-59-6
Solubility (25°C) DMSO: ≥10 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Frank Richter, et al. Transient Receptor Potential vanilloid 4 ion channel in C-fibres is involved in mechanonociception of the normal and inflamed joint

[2] Beatrix Pfanzagl, et al. The Transient Receptor Potential Vanilloid 4 Agonist RN-1747 Inhibits the Calcium Response to Histamine

[3] Nancy Stanslowsky, et al. Calcium, Sodium, and Transient Receptor Potential Channel Expression in Human Fetal Midbrain-Derived Neural Progenitor Cells

[4] R C L Vizin, et al. TRPV4 activates autonomic and behavioural warmth-defence responses in Wistar rats

[5] Fabien Vincent, et al. Identification and characterization of novel TRPV4 modulators

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