Cat. No.: HY-187975

MT-1207 free base

MT-1207 free base is an orally active, selective adrenergic α1 and 5-HT2A receptor antagonist. MT-1207 has IC₅₀ values of <0.1 nM, 0.15 nM, 1.40 nM, and 0.27 nM for α1A, α1B, α1D, and 5-HT2A, respectively. MT-1207 free base induces vasodilation, improves baroreflex sensitivity, and reduces heart rate in isolated hearts. MT-1207 free base lowers blood pressure, protects the heart, brain, and kidneys, improves cognition, delays stroke, reduces mortality, and lowers uric acid without impairing renal function in SHR/2K1C/2K2C models. MT-1207 free base exhibits high plasma protein binding, resistance to plasma esterases, and NADPH-dependent hepatic metabolism. MT-1207 free base can be used for research related to hypertension.

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

CAS No.: 917613-59-3
Formula: C₂₁H₂₄N₆S
Molecular Weight:392.52

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

MT-1207 free base Chemical Structure

CAS No.: 917613-59-3

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

^[1]

5-HT_2A Receptor

α1A-adrenergic receptor

0.1 nM (IC₅₀)

α1B-adrenergic receptor

0.15 nM (IC₅₀)

α1B-adrenergic receptor

1.40 nM (Ki)

α1D-adrenergic receptor

0.086 nM (IC₅₀)

α1D-adrenergic receptor

0.69 nM (Ki)

5-HT_2A Receptor

0.27 nM (IC₅₀)

5-HT_2A Receptor

0.079 nM (Ki)

All Adrenergic Receptor Isoforms :

All 5-HT Receptor Isoforms :

In Vitro

MT-1207 free base binds stably to α_1A, α_1B, α_1D, 5-HT_2A, 5-HT_2B, and 5-HT_2C receptors through hydrogen bonds, hydrophobic interactions, and van der Waals forces^[1].
MT-1207 (0.1 nM-1 μM) free base effectively inhibits adrenergic α_1A, α_1B, α_1D and 5-HT_2A receptors with high binding affinity^[3].
MT-1207 (1-100 nM; 60 min) free base is a potent multi-target antagonist of α1-adrenoceptor subtypes and 5-HT_2A receptors in CHO cell membranes^[2].
MT-1207 (10-1000 ng/mL; 30 min) free base exhibits extremely high plasma protein binding rates in Sprague-Dawley rat, beagle dog, cynomolgus monkey, and human plasma^[2].
MT-1207 (1 μg/mL; 0-120 min) free base exhibits strong plasma stability in human, Sprague-Dawley rat, Beagle dog, and cynomolgus monkey plasma, and is resistant to enzymatic hydrolysis by plasma esterases^[2].
MT-1207 (10 μM; 0-120 min) free base undergoes rapid NADPH-dependent metabolism in rat, beagle dog, cynomolgus monkey, and human liver microsomes^[2].
MT-1207 (0.2 ng/mL-2000 μg/mL; 20 min) free base does not significantly inhibit CYP3A4, CYP2C9, CYP1A2, and CYP2C19 in human liver microsomes, but exhibits a certain degree of CYP2D6 inhibition at higher concentrations^[2].

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

Parmacokinetics

Species	Dose	Route	T_1/2	T_max	C_max	AUC_0-t	V_{z-F_obs}	Cl_{F_obs}	F
Rat^[2]	1 mg/kg	i.v.	1.30 h	0.25 h	467.7 ng/mL	440.4 ng·h/mL	4.5 L	2.5 L/h	/
Rat^[2]	1 mg/kg	p.o.	1.50 h	0.16 h	33.3 ng/mL	51.7 ng·h/mL	51.5 L	23.3 L/h	11.7 %
Rat^[2]	3 mg/kg	p.o.	2.15 h	2.00 h	85.7 ng/mL	421.1 ng·h/mL	22.4 L	7.8 L/h	31.9 %
Rat^[2]	9 mg/kg	p.o.	1.89 h	0.65 h	185.8 ng/mL	605.4 ng·h/mL	78.9 L	35.2 L/h	15.3 %

In Vivo

MT-1207 (10 mg/kg/d; p.o.; daily; 9 weeks) free base significantly lowers BP in 2K2C rats without causing reflex HR increase^[1].
MT-1207 (10-20 mg/kg/d; p.o.; daily; 3 days to 9 weeks) free base reverses renal dysfunction and reduces uric acid levels in 2K2C rats^[1].
MT-1207 (10 mg/kg/d; p.o.; daily; 2 weeks) free base exerts uric acid-lowering effects in a hyperuricemia model^[1].
MT-1207 (10-20 mg/kg/d; p.o.; 9 weeks) free base ameliorates cognitive dysfunction in 2K2C rats^[1].
MT-1207 (10-20 mg/kg/d; p.o.; 9 weeks) free base exhibits cardiovascular and renal protective effects in 2K2C rats^[1].
MT-1207 (10 mg/kg/d; p.o.; lifelong) free base reduces mortality and extends lifespan in 2K2C rats^[1].
MT-1207 (1 mg/kg; i.v.) free base blocks α1 and 5-HT₂ receptors in vivo^[1].
MT-1207 (10 mg/kg/day; p.o.; 4 months) free base stably lowers blood pressure, improves baroreflex sensitivity, and provides renal and cardiovascular organ protection^[3].
MT-1207 (10 mg/kg/day; p.o.; approximately 8 months) stably lowers blood pressure free base and improves survival in stroke-prone SHR by delaying the onset of stroke and death^[3].
MT-1207 (10 mg/kg; p.o.; daily; 9 weeks) free base effectively lowers blood pressure without impairing renal function in the 2K2C renovascular hypertensive rat model^[2].
MT-1207 (2.5-10 mg/kg; p.o.; single dose) free base effectively lowers blood pressure in rats without causing the side effect of orthostatic hypotension^[2].
MT-1207 (250-1000 mg/kg; p.o.; single dose) free base is well tolerated in SD rats, with a maximum tolerated dose exceeding 1000 mg/kg^[2].
MT-1207 (10-100 mg/kg; p.o.; once daily; 13 weeks) free base is tolerated at all dose levels over 13 consecutive weeks, with a no-observed-adverse-effect level (NOAEL) of 100 mg/kg^[2].
MT-1207 (1.25-20 mg/kg; p.o.; single dose) free base produces a rapid, dose-dependent antihypertensive effect without inducing reflex tachycardia^[3].
MT-1207 (0.25-6 mg/kg; p.o.; single dose) free base dose-dependently lowers systolic blood pressure in 2K1C dogs, with effects maintained for over 12 h and without causing reflex tachycardia^[3].
MT-1207 (5 mg/kg/day; p.o.; once daily; for 7 consecutive days) free base significantly lowers systolic blood pressure and slightly slows heart rate without affecting ECG^[3].
MT-1207 (2 mg/kg/day; p.o.; once daily; for 7 consecutive days) free base significantly lowers systolic blood pressure and slightly slows heart rate, accompanied by minor ECG changes that recover after drug withdrawal^[3].

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

Animal Model:

Sprague Dawley (Male; 160-180 g)^[1]
Dosage:

10 mg/kg/d
Administration:

p.o.; daily; 4 and 9 weeks
Result:

Decreased systolic BP to 219 mmHg at the 4th week and 211 mmHg at the 9th week.
Showed a similar reducing effect on diastolic BP.
Had no significant effect on HR.

Animal Model:

Sprague Dawley (Male; 160-180 g)^[1]
Dosage:

10 mg/kg/d (acute); 10 and 20 mg/kg/d (long-term)
Administration:

p.o. (gavage); once a day; 3 days (acute); p.o. (drug-containing diet); 9 weeks (long-term)
Result:

Acute administration of MT (10 mg/kg/d) for 3 days decreased the serum uric acid level compared with the 2K2C model group, and it maintained serum creatinine, urea, and K+ concentrations at the same levels as sham-operated rats.
In the long-term experiment, MT did not deteriorate renal function in either group, but showed a significant uric acid-lowering effect compared with the 2K2C model group, and maintained serum K+ levels as sham-operated rats.

Animal Model:

Sprague Dawley (Male)^[1]
Dosage:

10 mg/kg/d
Administration:

p.o. (gavage); once a day; 2 weeks
Result:

Significantly reduced serum uric acid levels after 1 and 2 weeks of administration.

Animal Model:

Sprague Dawley (Male; 160-180 g)^[1]
Dosage:

10 and 20 mg/kg/d
Administration:

p.o. (drug-containing diet); 9 weeks
Result:

Both MT (10 and 20 mg/kg/d) long-term treatment groups were able to significantly reduce the swimming distance and latency, indicating an effect of improving the learning memory dysfunction in rats.
Two doses of MT showed different degrees of improvement in frequency of crossing the platform and the residence time in the target quadrant.

Animal Model:

Sprague Dawley (Male; 160-180 g)^[1]
Dosage:

10 and 20 mg/kg/d
Administration:

p.o. (test-article-containing diet); 9 weeks
Result:

Both MT (10 and 20 mg/kg/d) significantly improved cardiac and aortic hypertrophy.
The renal cortex to medulla thickness ratio in kidneys that did not undergo atrophy showed a slight improvement in the MT group.
The smaller kidney/larger kidney weight ratio in MT 10 mg/kg/d and 20 mg/kg/d groups showed different degrees of atrophy, and after MT treatment, the degree of atrophy was somewhat alleviated.
The incidence of atrophy was 60% in the MT 10 mg/kg/d group and 45.5% in the MT 20 mg/kg/d group.

Animal Model:

Sprague Dawley (Male; 160-180 g)^[1]
Dosage:

10 mg/kg/d
Administration:

p.o. (drug-containing diet); lifelong
Result:

Significantly prolonged the survival time of the rats, up to nearly 5 months.
Alleviated the continuous death of rats in the early stage and effectively reduced the death of animals.

Animal Model:

Sprague Dawley (Male; 160-180 g)^[1]
Dosage:

1 mg/kg
Administration:

i.v.; single administration
Result:

In rats with vehicle pre-treatment, phenylephrine induced a BP increase of about 90 mmHg, but this phenomenon totally disappeared in rats with MT pre-treatment.
Likewise, MT had an inhibitory effect on 2,5-dimethoxy-4-iodoamphetamine-induced BP increase.

Animal Model:

Sprague-Dawley (SD) (Male, 160-180 g, 2K2C renovascular hypertensive model)^[2]
Dosage:

10 mg/kg
Administration:

p.o.; daily; 9 weeks
Result:

Achieved a comparable antihypertensive effect to losartan (20 mg/kg), with systolic blood pressure (SBP) readings of 169 mmHg compared to approximately 202 mmHg in the 2K2C model rats.
Showed a tendency to decrease diastolic blood pressure (DBP) and did not elevate heart rate, instead causing a slight reduction.
Exhibited a minimal impact on urea, creatinine, and K+ levels, demonstrating excellent antihypertensive effects without damaging renal function in 2K2C rats.

Animal Model:

Sprague-Dawley (SD) (Male)^[2]
Dosage:

2.5, 5 and 10 mg/kg
Administration:

p.o.; single dose
Result:

Effectively lowered blood pressure after 30 min at 2.5, 5, and 10 mg/kg doses.
Displayed a consistent trend in blood pressure alteration when rats changed posture, with the maximum SBP reduction occurring at 5 s, ranging from 7 to 10 mmHg.
Varying degrees of SBP recovery were observed at 10 s.

Animal Model:

Sprague-Dawley (SD)^[2]
Dosage:

250-1000 mg/kg
Administration:

p.o.; single dose
Result:

No instances of unscheduled fatalities were recorded.
Rats in all groups displayed no discernible drug-related alterations in body weight or morphology.
Single oral administration at doses of 250, 500, and 1000 mg/kg in SD rats was well-tolerated, with the maximum tolerated dose (MTD) exceeding 1000 mg/kg.

Animal Model:

Sprague-Dawley (SD)^[2]
Dosage:

10, 30 and 100 mg/kg
Administration:

p.o.; once daily; 13 weeks
Result:

There were no unplanned mortalities in any of the groups.
No notable drug-related changes were revealed in morphological observations or post-mortem histopathological examinations.
In the 10 mg/kg group, rats did not exhibit any significant anomalies in body weight.
In the 30 mg/kg group, male rats showed a decrease in body weight on Day 11, with a weight reduction of approximately 3.3−7.2% during the dosing period, which gradually returned to normal post-cessation.
In the 100 mg/kg group, both male and female rats displayed decreased body weights on Day 4, with a weight decrease of approximately 5.4−14.7% in male rats and 3.3−6.8% in female rats, which also gradually returned to baseline levels after drug discontinuation.

Animal Model:

Spontaneously hypertensive rats (SHR) (male, 250 ± 20 g)^[3]
Dosage:

1.25, 2.5, 5, 10, 15, or 20 mg/kg
Administration:

i.g.; single dose
Result:

Decreased systolic blood pressure (BP) in all dose groups 15 min after administration.
Achieved maximal systolic BP decrease of 17 mmHg in the 1.25 mg/kg group and 21 mmHg in the 2.5 mg/kg group.
Achieved maximal systolic BP decrease of 41 mmHg in the 10 mg/kg group.
Demonstrated an obvious dose-effect relationship at 2.5, 5, and 10 mg/kg.
Decreased systolic BP by 12 mmHg at 2.5 min and 20 mmHg at 5 min after administration of 5 mg/kg.
Decreased BP significantly within 8-10 h after administration in 2.5, 5, and 10 mg/kg groups.
Did not increase heart rate but slightly decreased heart rate during BP reduction.

Animal Model:

Beagle dogs (male and female, 8-10 kg)^[3]
Dosage:

0.25, 0.5, 1, 1.5, 2, 4, or 6 mg/kg
Administration:

p.o. (gavage); single dose
Result:

Dose-dependently lowered systolic BP with a maximal reduction of 55 mmHg.
Decreased systolic BP by 14 mmHg at 5 min and by more than 20 mmHg at 10 min after administration of 2 mg/kg.
Showed a significant dose-effect relationship with the decrease in systolic and diastolic BP.
Maintained the decrease in systolic BP for more than 12 h.
Did not induce a reflex increase in heart rate but decreased heart rate.

Animal Model:

Spontaneously hypertensive rats (SHR) (male, 250 ± 20 g)^[3]
Dosage:

5 mg/kg/day
Administration:

p.o. (gavage); once daily; 7 consecutive days
Result:

Decreased average systolic BP from 175 ± 0.99 mmHg to 140 ± 2.43 mmHg.
Slightly slowed heart rate from 346 ± 21.88 bpm to 326 ± 16.39 bpm.
Had no significant effect on the ECG.

Animal Model:

Beagle dogs (male and female, 8-10 kg)^[3]
Dosage:

2 mg/kg/day
Administration:

p.o. (gavage); once daily; 7 consecutive days
Result:

Decreased average systolic BP from 173 ± 1.45 mmHg to 139 ± 1.38 mmHg.
Slightly slowed heart rate from 150 ± 3.66 bpm to 138 ± 4.75 bpm.
Prolonged the QT interval duration and QRS duration by 0.01 s and the T wave duration by 0.02 s on the 7th day.

Animal Model:

Spontaneously hypertensive rats (SHR) (male 350 ± 20 g and female 200 ± 20 g)^[3]
Dosage:

10 mg/kg/day
Administration:

p.o. (mixed in rat chow); 4 months
Result:

Decreased systolic BP by more than 20 mmHg 1 week after treatment and remained stable during 4 months.
Improved baroreflex sensitivity (BRS) to 0.53 ± 0.03 ms/mmHg compared with the vehicle control group (0.27 ± 0.01 ms/mmHg).
Significantly decreased glomerular sclerosis scores.
Improved pathological changes in the heart, brain and aorta.

Animal Model:

Stroke-prone spontaneously hypertensive rats (SHR-SP) (male, 350 ± 20 g)^[3]
Dosage:

10 mg/kg/day
Administration:

p.o. (mixed in rat chow); approximately 8 months
Result:

Decreased systolic BP by more than 20 mmHg and remained stable over 4 months.
Maintained stable heart rate with an average of 410 beats/min.
Improved the survival rate by delaying stroke occurrence and death.

Chemical Information

CAS No. 917613-59-3
Molecular Weight 392.52
Formula C₂₁H₂₄N₆S
SMILES

N1(CCCCN2CCN(CC2)C3=NSC4=C3C=CC=C4)N=NC5=C1C=CC=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Tian JS, et al. Pharmacological effects of MT-1207 in bilateral renal artery stenosis hypertension and its hypotensive targets validation. Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie. 2024 Sep;178:117234. [Content Brief]

[2]. Wang P, et al. Discovery of MT-1207: A Novel, Potent Multitarget Inhibitor as a Promising Clinical Candidate for the Treatment of Hypertension. Journal of medicinal chemistry. 2024 Sep 26;67(18):16128-16144. [Content Brief]

[3]. Xu TY, et al. Pharmacological characterization of MT-1207, a novel multitarget antihypertensive agent. Acta pharmacologica Sinica. 2021 Jun;42(6):885-897.

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MT-1207 free base

All Adrenergic Receptor Isoforms

All 5-HT Receptor Isoforms