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Hyp9

Cat. No. M7844
Hyp9 Structure
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Biological Activity

Sea foraminifen is the active ingredient of St. John's Wort. It has been used in studies of depression, is known to indirectly inhibit serotonin and norepinephrine reuptake at synapses, and has recently been found to work through direct activation of TRPC6. TRPC6 is a member of the typical transient receptor potential (TRPC) ion channel family. DAG is an endogenous activator of this pathway, and Hyperperforin is the only known selective activator of TRPC6. Although it is widely used, its chemical properties are unstable. Efforts to find a stable but pharmacologically similar activator of TRPC6 resulted in the discovery of a simplified phloroglucinol derivative Hyp9. Like hypericin, hypericin 9 inhibits serotonin reuptake and induces neurite growth. It increases the entry of calcium ions into the cell, selectively increasing the current through the TRPC6 channel.

Chemical Information
Molecular Weight 322.4
Formula C18H26O5
CAS Number 3118-34-1
Solubility (25°C) DMSO: ≥20 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] O Ajibola, et al. In silico characterisation of putative Plasmodium falciparum vaccine candidates in African malaria populations

[2] Lu Liu, et al. TRPC6 Attenuates Cortical Astrocytic Apoptosis and Inflammation in Cerebral Ischemic/Reperfusion Injury

[3] Li-Fen Zhou, et al. TRPC6 contributes to LPS-induced inflammation through ERK1/2 and p38 pathways in bronchial epithelial cells

[4] Qian Wang, et al. Local coupling of TRPC6 to ANO1/TMEM16A channels in smooth muscle cells amplifies vasoconstriction in cerebral arteries

[5] Dominique Yang, et al. Molecular mechanisms involved in LH release by the ovine pituitary cells

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Keywords: Hyp9 supplier, inhibitors, activators


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