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  2. Adenylate Cyclase PTHR
  3. TIP 39, Tuberoinfundibular Neuropeptide

TIP 39, Tuberoinfundibular Neuropeptide 

Cat. No.: HY-P1852 Purity: 99.83%
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TIP 39, Tuberoinfundibular Neuropeptide is an endogenous PTH2 receptor agonist and antihypertensive agent. TIP 39, Tuberoinfundibular Neuropeptide selectively activates the PTH2 receptor with no activity on the PTH1 receptor, stimulates cAMP production, activates adenylate cyclase, and elevates intracellular calcium levels via mobilization from intracellular stores. TIP 39, Tuberoinfundibular Neuropeptide is highly conserved in humans, mice, and rats. TIP 39, Tuberoinfundibular Neuropeptide is applicable to research related to nociception and inflammation-induced pain.

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

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TIP 39, Tuberoinfundibular Neuropeptide

TIP 39, Tuberoinfundibular Neuropeptide Chemical Structure

CAS No. : 277302-47-3

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Based on 1 publication(s) in Google Scholar

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1 Publications Citing Use of MCE TIP 39, Tuberoinfundibular Neuropeptide

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Description

TIP 39, Tuberoinfundibular Neuropeptide is an endogenous PTH2 receptor agonist and antihypertensive agent. TIP 39, Tuberoinfundibular Neuropeptide selectively activates the PTH2 receptor with no activity on the PTH1 receptor, stimulates cAMP production, activates adenylate cyclase, and elevates intracellular calcium levels via mobilization from intracellular stores. TIP 39, Tuberoinfundibular Neuropeptide is highly conserved in humans, mice, and rats. TIP 39, Tuberoinfundibular Neuropeptide is applicable to research related to nociception and inflammation-induced pain[1][2][3].

IC50 & Target

PTH2R

 

In Vitro

TIP 39, Tuberoinfundibular Neuropeptide stimulates arginine vasopressin release from in vitro rat hypothalamic explants[1].
TIP 39, Tuberoinfundibular Neuropeptide (log[ligand] M -13 to -6; 10 min) potently activate adenylyl cyclase to increase cAMP levels in HEK293 cells stably expressing human PTH2R, each with an EC50 of 0.2 nM[2].
TIP 39, Tuberoinfundibular Neuropeptide (log[ligand] M -11 to -5, 1 μM; acute addition) potently elevate intracellular calcium levels via mobilization from intracellular stores in HEK293 cells stably expressing human PTH2R, with EC50 values of 25 nM and 16 nM, respectively[2].
TIP 39, Tuberoinfundibular Neuropeptide (tested concentrations; 10 min) with N-terminal truncation reduces potency but retains full adenylyl cyclase activation efficacy in HEK293 cells stably expressing human PTH2R; C-terminal truncation to 30 or more residues retains full efficacy with reduced potency, while truncation to 29 residues eliminates activity[2].

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

In Vivo

TIP 39, Tuberoinfundibular Neuropeptide (100 pmol/rat; i.c.v.; single injection) produces a transient 44% reduction in basal plasma AVP levels in conscious rats, with maximum effect at 5 minutes post-injection[1].
TIP 39, Tuberoinfundibular Neuropeptide (100 pmol/rat; i.c.v.; single injection) produces a significant reduction in mean arterial pressure in conscious rats, with measurable effects at 20 minutes post-injection[1].
TIP 39, Tuberoinfundibular Neuropeptide (100 pmol/rat; i.c.v.; single injection) reduces dehydration-induced plasma AVP levels by 47.4% in conscious rats, with maximum effect at 5 minutes post-injection[1].
TIP 39, Tuberoinfundibular Neuropeptide (1-500 pmol/rat; i.c.v.; single injection) significantly suppresses dehydration-induced plasma AVP elevation in conscious rats, with a 32.7% reduction observed at 100 pmol/rat[1].
TIP 39, Tuberoinfundibular Neuropeptide (100 pmol/rat; i.c.v.; single injection) suppresses both hyperosmolality-induced and hypovolemia-induced plasma AVP elevation in conscious rats by 43.5% and 33.8%, respectively[1].
TIP 39, Tuberoinfundibular Neuropeptide (100 pmol/rat; i.c.v.; single injection) has an inhibitory effect on dehydration-induced plasma AVP release in conscious rats that is mediated by intrinsic opioid systems, as it is reversed by naloxone pretreatment[1].
TIP 39, Tuberoinfundibular Neuropeptide (10-100 pmol, 1.0 nmol; i.c.v.; single dose) partially reverses carrageenan-induced tactile allodynia at 10 and 100 pmol, reduces pain-related affective behavior at 1.0 nmol, and does not alter acute nociceptive responses in hot-plate or formalin tests in adult male Sprague-Dawley rats[3].

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

Animal Model: Sprague Dawley (male, 250-300 g)[1]
Dosage: 100 pmol/rat
Administration: i.c.v.; single injection
Result: Decreased plasma arginine vasopressin (AVP) levels to 0.70 pg/mL at 5 minutes post-injection.
Showed no significant decrease in plasma AVP at 15 minutes post-injection.
Left plasma Na+ and total protein levels unchanged.\nGradually decreased mean arterial pressure to 85.1 mm Hg at 20 minutes post-injection.
Animal Model: Sprague Dawley (male, 250-300 g, 48-hour water deprivation)[1]
Dosage: 100 pmol/rat
Administration: i.c.v.; single injection
Result: Suppressed dehydration-induced plasma AVP elevation to 4.32 pg/mL at 5 minutes post-injection.
Animal Model: Sprague Dawley (male, 250-300 g, 48-hour water deprivation)[1]
Dosage: 1 pmol/rat; 10 pmol/rat; 100 pmol/rat; 500 pmol/rat
Administration: i.c.v.; single injection
Result: Significantly suppressed dehydration-induced plasma AVP elevation at doses of 10, 100, and 500 pmol/rat.
Reduced plasma AVP levels to 4.64 pg/mL a 32.7% reduction, at 100 pmol/rat.
Left plasma Na+ and total protein levels unchanged.
Animal Model: Sprague Dawley (male, 250-300 g, hyperosmolality/hypovolemia induction)[1]
Dosage: 100 pmol/rat
Administration: i.c.v.; single injection
Result: Suppressed hyperosmolality-induced plasma AVP elevation to 2.65 pg/mL.
Suppressed hypovolemia-induced plasma AVP elevation to 4.10 pg/mL.
Left plasma Na+ and total protein levels unchanged.
Animal Model: Sprague Dawley (male, 250-300 g, 48-hour water deprivation, naloxone pretreatment)[1]
Dosage: 100 pmol/rat
Administration: i.c.v.; single injection
Result: Had its inhibitory effect on dehydration-induced plasma AVP elevation significantly reversed by pretreatment with naloxone, a nonselective opioid receptor antagonist.
Animal Model: Sprague-Dawley (adult male, 180-250 g; intraplantar lambda carrageenan-induced inflammatory pain)[3]
Dosage: 10 pmol; 100 pmol; 1.0 nmol
Administration: i.c.v.; single dose
Result: Did not significantly change paw withdrawal latency in hot-plate assay.
Did not significantly reduce pain scores in either phase 1 (0-10 minutes) or phase 2 (20-50 minutes) of formalin test.
Partially reversed carrageenan-induced tactile hypersensitivity 2 minutes post-administration at 10 pmol and 100 pmol; this effect was absent by ~40 minutes post-administration.
Did not significantly affect tactile withdrawal threshold at 1.0 nmol.
Significantly decreased the escape/avoidance response (time spent in the light chamber side) to stimulation of the inflamed paw at 1.0 nmol; an apparent effect was observed with the 100 pmol dose, while the 10 pmol dose showed no significant difference from vehicle.
Molecular Weight

4504.20

Formula

C202H325N61O54S

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Ser-Leu-Ala-Leu-Ala-Asp-Asp-Ala-Ala-Phe-Arg-Glu-Arg-Ala-Arg-Leu-Leu-Ala-Ala-Leu-Glu-Arg-Arg-His-Trp-Leu-Asn-Ser-Tyr-Met-His-Lys-Leu-Leu-Val-Leu-Asp-Ala-Pro

Sequence Shortening

SLALADDAAFRERARLLAALERRHWLNSYMHKLLVLDAP

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (11.10 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.2220 mL 1.1101 mL 2.2201 mL
5 mM 0.0444 mL 0.2220 mL 0.4440 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.84%

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 (sealed storage, away from moisture). 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
H2O 1 mM 0.2220 mL 1.1101 mL 2.2201 mL 5.5504 mL
5 mM 0.0444 mL 0.2220 mL 0.4440 mL 1.1101 mL
10 mM 0.0222 mL 0.1110 mL 0.2220 mL 0.5550 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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.

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TIP 39, Tuberoinfundibular Neuropeptide
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